bluuebunny/crossref_metadata_2025 huggingface dataset:
Endovascular Management of Intracranial Aneurysms: Current Experience and Future Advances
Authors: Koebbe Christopher J. , Veznedaroglu Erol , Jabbour Pascal , Rosenwasser Robert H.
Published: October 2006

OBJECTIVE:

The past 15 years have seen a revolution in the treatment of intracranial aneurysms. Endovascular technology has evolved rapidly since the Food and Drug Administration approval of Guglielmi detachable coils in 1995, which now allows successful treatment of most aneurysms. The authors provide a review of their 11-year experience at Jefferson Hospital for Neuroscience with endovascular embolization of intracranial aneurysms and discuss clinical trial outcomes and future directions of this treatment method.

METHODS:

The authors reviewed the clinical and angiographic outcomes for 1307 patients undergoing endovascular treatment of intracranial aneurysms. Their analysis focuses on posterior circulation and middle cerebral artery aneurysms, as well as cases of stent-assisted coil embolization. They review their procedural protocol and patient selection criteria for endovascular management.

RESULTS:

Several large clinical trials have demonstrated the safety and efficacy of endovascular treatment of intracranial aneurysms. The International Subarachnoid Aneurysm Trial provides Level I evidence demonstrating a significant reduction in disability or death with endovascular treatment compared with surgical clipping. The most common procedural complications include intraprocedural rupture and thromboembolic events; avoidance strategies are also discussed. Vasospasm after subarachnoid hemorrhage causes neurological morbidity and mortality and can be successfully managed by early recognition and interventional treatment with angioplasty, pharmacologic agents, or both.

CONCLUSION:

Long-term studies evaluating experience with aneurysm coil embolization during the past decade indicate that this is a safe and durable treatment method. The introduction of stent-assist techniques has improved the management of wide-neck aneurysms. Future technology developments will likely improve the durability of endovascular treatment further by delivering bioactive agents that promote aneurysm thrombosis beyond the coil mass alone. It is clear that endovascular therapy of both ruptured and unruptured aneurysms is becoming a mainstay of practice in this patient population. Although not replacing open surgery, the continued improvements have allowed aneurysms that previously were amenable only to open clip ligation to be treated safely with durable long-term outcomes.
Penetrating neck wounds: Selective exploration.
Authors: May Mark , Chadaratana Phadung , West Joseph W. , Ogura Joseph H.
Published: October 2006

This study of 223 patients with penetrating neck wounds justifies individualizing surgical treatment. Twenty‐four percent was selected for neck surgery. In spite of selective rather than mandatory neck exploration, the mortality rate related to the neck wound in this series was three percent. This compared favorably with the experience of others employing mandatory exploration. There were no deaths in our series attributable to selective observation.
Otologic history, audiometry and tympanometry as a case finding procedure for school screening
Authors: Beery Quinter C. , Bluestone Charles D. , Cantekin Erdem I.
Published: October 2006

An algorithm for identification of hearing loss and middle ear effusion based on otologic history, audiometry and tympanometry was designed and tested on 771 first grade school children. Each ear was profiled as being normal, at risk, at high risk, or in need of otologic referral based on test‐retest screening. In addition, each child was categorized on the basis of the worse ear. Results showed 57 percent of the children as being normal; otologic referral was indicated in 14 percent. The remaining children (29 percent) were at risk or at high risk. The combination of medical history, audiometry and tympanometry constitutes an excellent case finding procedure for screening the otologic status of young school children. Through the utilization of specific criteria, optimal referrals can be made, thereby providing better health care.
Primary monomorphic adenoma of the middle ear
Authors: Hagan Warren E. , Leonard George L. , Ichinose Herbert , Cox Robert H.
Published: October 2006

The benign, monomorphic adenoma, derived from the respiratory epithelium of the middle ear, is a well circumscribed, greyish, avascular tumor. Its histology — documented by light and electron micrographs contained in this report — supports a distinct entity and pathogenesis apart from the malignant adenocarcinoma. Utilizing two case reports, this compendium emphasizes the clinical presentations, as well as radiographic and audiometrical characteristics, of the tumor. The first case represents the typical tumor with conductive hearing loss. The second case is the first reported facial paralysis associated with hemorrhagic infarction of an adenoma which was reversible by surgical resection of the tumor. Based on the histology and four year postoperative follow‐up, the authors conclude the adenoma may be effectively managed by surgical resection.
Significance of tomography in meniere's disease: Periaqueductal pneumatization
Authors: Hall Stephen F. , O'Connor A. Fitzgerald , Thakkar C. H. , Wylie I. G. , Morrison A. W.
Published: October 2006

The revival of endolymphatic sac surgery has led to many investigations in Meniere's disease, including lateral tomography of the periaqueductal pneumatization. We radiologically assessed a series of Meniere's patients and a control group, and found hypocellularity to be more common in Meniere's disease as the literature has stated. However, we found this finding bilaterally in patients with unilateral disease. Our assessment of this information in regard to the etiology and treatment of Meniere's disease is presented.
Ventilation tube surgery and middle ear irrigation
Authors: Balkany Thomas J. , Kaufman Arenberg I. , Steenerson Ronald Leif
Published: October 2006

Tympanostomy and insertion of ventilation tubes has become one of the most commonly performed operations in the United States. Most authors reporting complications of this procedure describe a postoperative rate of otorrhea in the range of 10%–20% with some reports much higher. This rate of presumed suppuration would generally be considered high by surgeons operating in other areas of the body.

It is a commonly accepted surgical practice to follow incision and drainage of a relatively closed space effusion with irrigation of that space. This is true in the surgery for the paranasal sinuses, deep space infections of the neck, joint spaces, and abscesses in general. However, this practice is not routinely performed when incising and draining the middle ear.

We have completed a prospective controlled double blind study on post‐tympanostomy tube otorrhea utilizing irrigation of the middle ear. In 220 consecutive cases, the use of middle ear irrigation reduced postoperative infections in the first 6 months from 16% to 4%. Irrigation was also found to be useful in removing very thick effusions from the middle ear by displacement, including those effusions localized in the hypo or epitympanum which were not initially identified at the time of incision and suction. A soft plastic, angled irrigation catheter with radial ports was developed for this purpose.
Complications following reconstruction with the pectoralis major myocutaneous flap: The effect of prior radiation therapy
Authors: Keidan Richard D. , Kusiak Joseph F.
Published: October 2006

Over the past 5 years, 40 patients with head and neck cancer underwent pectoralis major myocutaneous flap (PMMF) reconstruction following radical ablative surgery. Twenty‐three patients received prior radiation therapy (55 to 70.2 Gy), while 17 patients had no radiation preoperatively. Thirty‐five percent of the irradiated patients had flap‐related complications, compared to 47% of the nonirradiated patients (P = .52, not statistically significant [NSS]). There were no reoperations and no operative deaths in either group. There was 1 fistula in each group, both of which closed with conservative management. The PMMF for head and neck reconstruction is well tolerated following radiation therapy and has shown comparable morbidity in patients who have not undergone prior radiation.
The role of early tracheotomy in the management of the neurosurgical patient
Authors: Boyd Susan Webb , Benzel Edward C.
Published: October 2006

Neurosurgical patients often require prolonged laryngeal intubation. The literature regarding the management of these patients is controversial, with some series reporting increased benefits of early tracheotomy and others reporting similar benefits of prolonged transtracheal intubation. One hundred sixteen consecutive neurosurgical patients who had tracheotomies performed during a 5‐year period are presented in order to clarify some of the factors involved with these issues.

The complications that occurred in this series were less frequent than those reported in most of the published series. Of the 116 patients, 7 had posttracheotomy complications. These complications included stomal infections (4 patients), hemorrhage (1 patient), subglottic granulation tissue (1 patient), and tracheitis (1 patient). All complications were easily treated and caused no significant long‐term morbidity. Furthermore, pulmonary care was universally facilitated by the placement of a tracheotomy.

The performance of an early postinjury tracheotomy may prevent the known complications of prolonged endotracheal intubation while providing effective ventilation and pulmonary toilet through safe and comfortable access to the airway. Early postinjury tracheotomy is not associated with a high incidence of significant complications in the neurosurgical patient population.
Electrical promontory stimulation in patients with intact cochlear nerve and anacusis following acoustic neuroma surgery
Authors: Cueva Roberto A. , Thedinger Britt A. , Harris Jeffrey P. , Glasscock Michael E.
Published: October 2006

Anacusis following hearing preservation surgery for acoustic neuroma removal in which the cochlear nerve was preserved has been explained on the basis of neural or vascular compromise. In the absence of pathologic evidence for either theory, a physiologic model was chosen. Electrical promontory stimulation with monitoring of subjective and electrically evoked auditory brainstem responses was undertaken. A positive response to stimulation suggests a vascular impairment of the cochlea sparing the cochlear nerve and spiral ganglion. The absence of response suggests loss of neural integrity at the level of the spiral ganglion or cochlear nerve. Six patients who suffered anacusis following hearing preservation surgery for acoustic neuroma were studied. Data regarding electrical promontory stimulation, auditory brainstem responses, and implications of the possible role of cochlear implantation are discussed.
The role of guaifenesin in the treatment of sinonasal disease in patients infected with the human immunodeficiency virus (HIV)
Authors: Wawrose Stephen F. , Tami Thomas A. , Amoils C. Phillip
Published: October 2006

Inflammatory sinonasal disease is a common problem in patients infected with the human immunodeficiency virus (HIV). Although some patients present with acute or chronic sinusitis, many describe persistent nasal congestion and thick, tenacious postnasal drainage, even in the absence of infection. The efficacy of guaifenesin as a mucolytic is poorly documented and support for its use in this setting is primarily anecdotal. This double‐blind, placebo‐controlled study assessed changes in nasal symptoms among 23 HIV‐infected patients receiving either 3 weeks of guaifenesin (2400 mg daily) or placebo. The guaifenesin group reported less nasal congestion and thinner postnasal drainage compared to the placebo group and these differences were statistically significant (P <.05). Guaifenesin appears to be effective in managing HIV‐infected patients with symptomatic rhinosinusitis and may be a useful adjunct for treating acute and chronic sinusitis in this population.
Blockade of Adenosine A2AReceptors Prevents Protein Phosphorylation in the Striatum Induced by Cortical Stimulation
Authors: Quiroz César , Gomes Catarina , Pak Arlene C. , Ribeiro Joaquim A. , Goldberg Steven R. , Hope Bruce T. , Ferré Sergi
Published: October 2006

Previous studies have shown that cortical stimulation selectively activates extracellular signal-regulated kinase 1/2 (ERK1/2) phosphorylation and immediate early gene expression in striatal GABAergic enkephalinergic neurons. In the present study, we demonstrate that blockade of adenosine A2Areceptors with caffeine or a selective A2Areceptor antagonist counteracts the striatal activation of cAMP–protein kinase A cascade (phosphorylation of the Ser845residue of the glutamate receptor 1 subunit of the AMPA receptor) and mitogen-activated protein kinase (ERK1/2 phosphorylation) induced by thein vivostimulation of corticostriatal afferents. The results indicate that A2Areceptors strongly modulate the efficacy of glutamatergic synapses on striatal enkephalinergic neurons.
Subthalamic Stimulation-Induced Forelimb Dyskinesias Are Linked to an Increase in Glutamate Levels in the Substantia Nigra Pars Reticulata
Authors: Boulet Sabrina , Lacombe Emilie , Carcenac Carole , Feuerstein Claude , Sgambato-Faure Véronique , Poupard Annie , Savasta Marc
Published: October 2006

The neurobiological mechanisms by which high-frequency stimulation of the subthalamic nucleus (STN–HFS) alleviates the motor symptoms of Parkinson's disease (PD) remain unclear. In this study, we analyzed the effects of STN–HFS on motor behavior in intact or hemiparkinsonian rats (6-hydroxydopamine lesion of the substantia nigra pars compacta) and investigated the correlation between these effects and extracellular glutamate (Glu) and GABA levels, assessed by intracerebral microdialysis in the substantia nigra pars reticulata (SNr). STN–HFS at an intensity corresponding to the threshold inducing contralateral forelimb dyskinesia, increased Glu levels in the SNr of both intact and hemiparkinsonian rats. In contrast, STN–HFS at half this intensity did not affect Glu levels in the SNr in intact or hemiparkinsonian rats but increased GABA levels in hemiparkinsonian rats only. STN–HFS-induced forelimb dyskinesia was blocked by microinjection of the Glu receptor antagonist kynurenate into the SNr and facilitated by microinjection of a mixture of the Glu receptor agonists AMPA and NMDA into the SNr. These new neurochemical data suggest that STN–HFS-induced forelimb dyskinesia is mediated by glutamate, probably via the direct activation of STN axons, shedding light on the mechanisms of STN–HFS in PD.
Inositol 1,4,5-Trisphosphate Receptor Type 1 in Granule Cells, Not in Purkinje Cells, Regulates the Dendritic Morphology of Purkinje Cells through Brain-Derived Neurotrophic Factor Production
Authors: Hisatsune Chihiro , Kuroda Yukiko , Akagi Takumi , Torashima Takashi , Hirai Hirokazu , Hashikawa Tsutomu , Inoue Takafumi , Mikoshiba Katsuhiko
Published: October 2006

Here, we show that cultured Purkinje cells from inositol 1,4,5-trisphosphate receptor type 1 knock-out (IP3R1KO) mice exhibited abnormal dendritic morphology. Interestingly, despite the huge amount of IP3R1 expression in Purkinje cells, IP3R1 in granule cells, not in the Purkinje cells, was responsible for the shape of Purkinje cell dendrites. We also found that BDNF application rescued the dendritic abnormality of IP3R1KO Purkinje cells, and that the increase in BDNF expression in response to activation of AMPA receptor (AMPAR) and metabotropic glutamate receptor (mGluR) was impaired in IP3R1KO cerebellar granule cells. In addition, we observed abnormalities in the dendritic morphology of Purkinje cells and in the ultrastructure of parallel fiber–Purkinje cell (PF-PC) synapses in IP3R1KO micein vivo. We concluded that activation of AMPAR and mGluR increases BDNF expression through IP3R1-mediated signaling in cerebellar granule cells, which contributes to the dendritic outgrowth of Purkinje cells intercellularly, possibly by modifying PF-PC synaptic efficacy.
Marriage: The Good, the Bad, and the Greedy
Authors: Gerstel Naomi , Sarkisian Natalia
Published: October 2006

Even good marriages can have some bad side effects, taking people away from other social connections.
Parents, Adult Children, and Immortality
Authors: Umberson Debra
Published: October 2006

As we live longer, most of us maintain relationships with our parents into middle age and beyond. How do these connections affect our health and well-being?
Waste Not, Want Not: Excrement and Economy in Nineteenth-Century France
Authors: SIMMONS DANA
Published: October 2006

ABSTRACT In mid-nineteenth-century France, the science of animal nutrition morphed into a Romantic political program. Scientists and socialists formulated a kind of industrial physiocracy that sought to replace wage work and finance capital with an unimpeded flow of excrement.
An elutriation apparatus for assessing settleability of combined sewer overflows (CSOs)
Authors: Marsalek J. , Krishnappan B.G. , Exall K. , Rochfort Q. , Stephens R.P.
Published: October 2006

An elutriation apparatus was proposed for testing the settleability of combined sewer outflows (CSOs) and applied to 12 CSO samples. In this apparatus, solids settling is measured under dynamic conditions created by flow through a series of settling chambers of varying diameters and upward flow velocities. Such a procedure reproduces better turbulent settling in CSO tanks than the conventional settling columns, and facilitates testing coagulant additions under dynamic conditions. Among the limitations, one could name the relatively large size of the apparatus and samples (60 L), and inadequate handling of floatables. Settleability results obtained for the elutriation apparatus and a conventional settling column indicate large inter-event variation in CSO settleability. Under such circumstances, settling tanks need to be designed for “average” conditions and, within some limits, the differences in test results produced by various settleability testing apparatuses and procedures may be acceptable. Further development of the elutriation apparatus is under way, focusing on reducing flow velocities in the tubing connecting settling chambers and reducing the number of settling chambers employed. The first measure would reduce the risk of floc breakage in the connecting tubing and the second one would reduce the required sample size.
Assessment of WWTP design and upgrade options: balancing costs and risks of standards' exceedance
Authors: Benedetti L. , Bixio D. , Vanrolleghem P.A.
Published: October 2006

Numerical models can be used to evaluate design and upgrade scenarios of urban wastewater systems on the basis of their ecological consequences. The objective of this paper is to illustrate a systematic procedure of system design/upgrade. This procedure consists of the following steps: (1) data collection and data reconstruction; (2) model building and calibration; (3) evaluation of scenarios; (4) uncertainty assessment. In contrast to conventional practice, this approach allows to choose the most appropriate trade-off between cost of measures and risk of non-compliance with regulatory limits. An example of its application dealing with the assessment of WWTP design and upgrade options is provided. Results show that by reducing the tank volumes compared to conventional design procedures, costs can be reduced sensibly while the risk of not meeting legislative requirements are only slightly increased.
Prolonged deposition of heavy metals in infiltration facilities and its possible threat to groundwater contamination
Authors: Aryal R.K. , Murakami M. , Furumai H. , Nakajima F. , Jinadasa H.K.P.K.
Published: October 2006

A field investigation of infiltration facilities, built two decades ago in Tokyo, was carried out and sediment samples were collected from 12 infiltration inlets of three different locations. Heavy metals contents in the inlet sediment, road dusts and soils samples were analysed and compared. The particle size distribution analysis showed its variation in depth as well as from inlet to inlet. The nature of organic substances present in sediment found changes in particle sizes as well as in depth. The heavy metals content in the sediment samples ranged from 6–143 (Cr), 1–84 (Ni), 49–331 (Cu), 210–2186 (Zn) and 2–332 (Pb) μg/g. The heavy metal content ranges were similar to road dust, which indicated road dust as a possible source for sediment for the infiltration inlets. The lower heavy metals content in many sediment samples than the soil indicated possible release/desorption of heavy metals under newly created environments such as an anaerobic environment. Among the heavy metals there was a relatively good relationship between Cu and Zn, indicating the existence of their common sources.
Integrated modelling of two xenobiotic organic compounds
Authors: Lindblom E. , Gernaey K.V. , Henze M. , Mikkelsen P.S.
Published: October 2006

This paper presents a dynamic mathematical model that describes the fate and transport of two selected xenobiotic organic compounds (XOCs) in a simplified representation of an integrated urban wastewater system. A simulation study, where the xenobiotics bisphenol A and pyrene are used as reference compounds, is carried out. Sorption and specific biological degradation processes are integrated with standardised water process models to model the fate of both compounds. Simulated mass flows of the two compounds during one dry weather day and one wet weather day are compared for realistic influent flow rate and concentration profiles. The wet weather day induces resuspension of stored sediments, which increases the pollutant load on the downstream system. The potential of the model to elucidate important phenomena related to origin and fate of the model compounds is demonstrated.
Assessment of CSO loads – based on UV/VIS-spectroscopy by means of different regression methods
Authors: Hochedlinger M. , Kainz H. , Rauch W.
Published: October 2006

The use of UV/VIS-spectroscopy for water quality measurements is based on the solution of the correlation between the surrogate parameter absorbance and the resulting equivalence parameters. The coherence of absorbance and equivalence parameters (CODtot, CODsol, TSS) is solved in this paper with different regression methods. The correlation of absorbance and concentrations are analysed based on linear regression methods, model tree regressions, multivariate regression methods and support vector machines using sequential minimal optimisation algorithm. For this purpose the regression methods are calibrated on three 24hours measurement campaigns of a combined sewer measurement station situated in the combined sewer overflow chamber in Graz (Austria). The online measurement station has been conveying data for more than 2½ years up to now. Finally, the load calculation based on the different regression methods and its comparison demonstrate that an apparently complex model does not inevitably lead to accurate concentration values due to possible model overfitting. Hence, the paper points out the possibilities and the drawbacks of spectroscopy measuring in sewers and the arising concentration values.
PERCEPTIONS OF COLLEGE WOMEN WITH DISORDERED EATING AND EXERCISE PATTERNS
Authors: Johnstone Jessica R. , Rickard Kathryn M.
Published: October 2006

This study examined college students' perceptions of women struggling with various eating-and exercise-related disorders. The 220 participants read a vignette describing either an anorexic female, a bulimic female, a female who engages in excessive exercise, or a control female
target. The targets were rated on a list of personality and physical dimensions. The participants' demographic information, perceived similarity to the target, and experience with someone similar to the target were also examined. Results demonstrated that the targets with anorexia and
bulimia were viewed significantly more negatively than were excessive exercising and control targets. Perceived personal similarity to the target also significantly increased positive ratings of the targets, which suggests that those who have had an eating disorder may empathize with those
who are currently struggling.
Antimicrobial susceptibility patterns of respiratory tract pathogens from sheep and goats
Authors: Berge Anna Catharina B. , Sischo William M. , Craigmill Arthur L.
Published: October 2006

Objective—To determine the antimicrobial susceptibility of common respiratory tract pathogens from sheep and goats.

Design—Cross-sectional study.

Sample Population—41 respiratory tract isolates from sheep and 36 isolates from goats.

Procedures—Disk diffusion assay was used to determine antimicrobial susceptibility of isolates to amoxicillin-clavulanic acid, ceftiofur, ciprofloxacin, florfenicol, and tetracycline. Minimum inhibitory concentrations of florfenicol for these isolates were determined by use of the microbroth dilution technique.

Results—The most common isolates were Pasteurella multocida (n = 28) and Mannheimia haemolytica (39). All isolates were susceptible to amoxicillin-clavulanic acid, ceftiofur, ciprofloxacin, and florfenicol. Five percent (4/77) of isolates were resistant to tetracycline.

Conclusions and Clinical Relevance—Susceptibility of respiratory tract pathogens isolated from sheep and goats to commonly used antimicrobial drugs in this study was high. Treatment of these species for bacterial respiratory tract disease is likely not complicated by antimicrobial resistance.
Smart blending technology enabled by chaotic advection
Authors: Zumbrunnen D. A. , Subrahmanian R. , Kulshreshtha B. , Mahesha C.
Published: October 2006

Polymer blending has been typically regarded as a mixing process rather than a structuring process so polymer blends and composites are not necessarily optimized with regard to structure, properties, and composition. In this article, a new smart blending technology is described whereby melt components and solid additives are more controllably organized into micrometer‐scale and sub‐micrometer‐scale shapes and arrangements to improve properties or impart functionality to extruded plastics. Chaotic advection is an enabling recent subfield of fluid mechanics for smart blending. It provides a method to controllably stretch and fold melt domains and evolve a multilayered structure leading to derivative morphologies, or indirectly manipulate solid additives. Recent advances in fluid mechanics have thereby been implemented to reconsider how blending is done. A variety of structured plastic materials are producible with a single smart blending device with no device alterations. Several examples and their improved physical properties are shown or discussed. © 2006 Wiley Periodicals, Inc. Adv Polym Techn 25:152–169, 2006; Published online in Wiley InterScience (www.interscience.wiley.com). DOI 10.1002/adv.20073
Role of drug efflux carriers in the healthy and diseased brain
Authors: Hermann Dirk M. , Kilic Ertugrul , Spudich Annett , Krämer Stefanie D. , Wunderli‐Allenspach Heidi , Bassetti Claudio L.
Published: October 2006

The blood–brain barrier is a natural diffusion barrier, which expresses active carriers extruding drugs on their way to the brain back into the blood against concentration gradients. Whereas these so‐called adenosine triphosphate–binding cassette (ABC) transporters prevent the brain entry of toxic compounds under physiological conditions, they complicate pharmacotherapies in neurological disease. Recent observations in animal models of ischemic stroke, drug‐resistant epilepsy, and brain cancer showed that the prototype of ABC transporters, ABCB1, is upregulated on brain injury, deactivation of this carrier considerably enhancing the accumulation of neuroprotective, antiepileptic, and chemotherapeutic compounds. These studies provide the proof of concept that the efficacy of brain‐targeting drugs may significantly be improved when drug efflux is blocked. Under clinical conditions, efforts currently are made to enhance drug accumulation by selecting new compounds that do not bind to efflux carriers or deactivating ABC transporters by targeted downregulation or pharmacological inhibition. We predict that strategies aiming at circumventing drug efflux may greatly facilitate progress in neurological therapies. Ann Neurol 2006
Boran‐Addukte des Narkotins und Hydrastins und ihrer Reduktionsprodukte
Authors: Prior Silvia , Wiegrebe Wolfgang
Published: October 2006

α‐Narkotin (3), β‐Hydrastin (6) und ihre Reduktionsprodukte binden Boran koordinativ am Stickstoff. — Aus α‐Narkotindiol (8) entsteht mit K‐tert. butylat/Benzophenon nicht α‐Anhydronarkotindiol7), sondern eine Quettamin‐ähnliche Verbindung 9 ohne Racemisierung am Benzyl‐C.
Synthesis of 6‐Substituted 2‐Phenyl‐3‐(5‐substituted mercapto‐1,3,4,thiadiazol‐2‐yl)quinazolin‐4‐(3H)‐ones as Antitubercular Agents
Authors: Kumar Piyush , Dhawan Keshav N. , Vrat Satya , Bhargava Krishna P. , Kishore Kesari
Published: October 2006

2‐Amino‐5‐mercapto‐1,3,4‐thiadiazole was condensed with various 6‐substituted 2‐phenylbenzoxazin‐4 (3H)‐ones to yield the compounds 1. When these compounds were subjected to mercaptoetherification the title compounds 2–4 were obtained. They were screened for their antitubercular activity against Mycobacterium smegmatis and Mycobacterium tuberculosis H37 Rv in vitro. Structure‐activity relationships were established.
Synthese von Leukotrien E3
Authors: Spur Bernd , Falsone Gioacchino , Crea Attilio , Peters Wilfried , König Wolfgang
Published: October 2006

Die Synthese von Leukotrien E3 (5b) sowie von Leukotrien C3 (6b) und Leukotrien D3 (7b) aus Leukotrien A3 (3) wird beschrieben.
Photo‐Akustische Spektroskopie in der Pharmazie
Authors: Stahl Egon , Breuer Hans Dieter
Published: October 2006

Zur farblichen Bewertung von Drogenpulvern und Carotinoiden werden Remissionsspektren mit photo‐akustischen Spektren (PAS) verglichen. Mit einem Eigenbaugerät werden Messungen im Bereich zwischen 350 und 750 nm bei einer Chopperfrequenz von 415 Hz durchgeführt. Wie die abgebildeten Spektren zeigen, ist die PAS der Remissionsspektroskopie deutlich überlegen.
Zum Schmelzverhalten hydratisierter tensidhaltiger Suppositoriengrundlagen
Authors: Fischer Wilfried , Knie Ulrich
Published: October 2006

In Mischungen von Witepsol® W 35

WZ der Firma Dynamit Nobel, Witten.

mit Tween® 60

WZ der Firma Atlas Chemie, Essen.

treten nach Zusatz geringer Wassermengen flüssig‐kristalline Phasen auf, deren Schmelzpunkt bei 46° liegt. Diese Mesophasen verleihen den Suppositorienmassen unerwünschte Eigenschaften wie erhöhte Viskosität bei Körpertemperatur, Solubilisierung von Arzneistoffen und können unter Umständen die Resorption von Arzneistoffen behindern. Nicht hydroxylhaltiges Hartfett (Witepsol® H 35) zeigt dieses Verhalten nicht. Aus diesem Unterschied wird auf eine aktive Beteiligung der hydroxylhaltigen Hartfettmasse an der vermutlich lamellaren Struktur der Mesophasen geschlossen.
Analyse des Ammoniumbituminosulfonates Ichthyol®
Authors: Koch Jürgen , Moser Reinhold , Demel Johann
Published: October 2006

Von unsulfonierten Anteilen befreites Ichthyol® (Ammoniumbituminosulfonat DAB 8) wurde nach Fraktionierung mittels Anionenaustauscher und Kieselgel‐DC in die freien Sulfonsäuren überführt und anschließend zu den Sulfonsäuremethylestern und Sulfonylfluoriden umgesetzt. In den Derivaten wurden mit Hilfe kombinierter GC/MS 20 homologe Reihen von z. T. schwefelhaltigen Alkylaromaten mit insgesamt 126 Einzelverbindungen im Mol.‐Massenbereich von ca. 170 bis 420 identifiziert, die im allgemeinen jeweils in Form mehrerer Stellungsiomere auftreten. Ferner wurden Hinweise auf weitere aromatische Grundkörper erhalten und verschiedene Fettsäuren nachgewiesen.
Regiospezifische Synthese von 2‐Phenyl‐pyrano[3,4‐b]pyranonen (Oxaflavon‐Derivaten) mit Tetrahydro‐3‐pyranon
Authors: Eiden Fritz , Wanner Klaus Th.
Published: October 2006

Tetrahydro‐3‐pyranon (5) reagiert unter definierten Bedingungen mit Trimethylsilylchlorid regiospezifisch zum Enolether 6. Nach Spaltung mit Methyllithium und Reaktion mit Zimtsäurechlorid entsteht daraus das 4‐Cinnamoylpyranon 8. Protonenkatalysierter Ringschluß und DDQ‐Dehydrierung liefern die Pyrano[3,4‐b]pyranone 9 bzw. 10.
Partialsynthese neuer Ergolinderivate aus Clavinalkaloiden, 4. Mitt. N‐1‐, C‐2‐ und N‐6‐monosubstituierte Agroclavine
Authors: Eich Eckart , Sieben Reinhold , Becker Christoph
Published: October 2006

Agroclavin (1) wird in flüssigem Ammoniak/Kaliumamid mit Alkyliodid am Indolstickstoff alkyliert. 1 läßt sich mit N‐Iodsuccinimid zu 2‐Iod‐1 (3) umsetzen. Mit der Bromcyan‐Methode wird 6‐Nor‐1 (4b) gewonnen und danach an N‐6 alkyliert.
Herstellung und Eigenschaften von β‐Ketopropansultonen und ‐sultamen
Authors: Stachel Hans‐Dietrich , Drasch Gustav
Published: October 2006

Durch Dieckmann‐Kondensation wurden die 1,2‐Oxathiolan‐4‐on‐2,2‐dioxide 5 und Isothiazolidin‐4‐on‐1,1‐dioxide 6 hergestellt. Alle Verbindungen besitzen pKs‐Werte um 4. Bemerkenswert ist die große Alkalistabilität insbesondere der Sultone 5.
Darstellung und Reaktionen von 2‐Acetyl‐3‐amino‐5‐hydroxy‐2‐cyclohexenonen; Benzol‐Derivate aus Pyronen
Authors: Eiden Fritz , Patzelt Gertrud
Published: October 2006

Das 3‐Acetylpyron 2 reagiert mit den sek. Aminen 3a–3k zu den Aminocyclohexenonen 5a–5g und 8 bzw. den Aminophenolen 7h und 7i; Ammoniak und o‐Phenylendiamin dagegen bilden die Tetrahydropyridinone 11a und 11b bzw. das Dihydropyridin 12. In 5a läßt sich die Aminogruppe durch Ammoniak, Amine, Aminosäuren bzw. Hydrazin‐Derivate austauschen, wobei 14a, 14c, 14e–14g entstehen; mit Benzamidin bzw. Hydrazinen reagiert 5a zum Tetrahydrochinazolin 21 bzw. den Tetrahydroindazolen 24a und 24b. Die Cyclohexenon‐Derivate 5, 8, 14, 21 und 24 werden bei Einwirkung von Kaliumhydroxid in Ethanol dehydratisiert, wobei die Phenol‐Derivate 7a–7h, 9, 15a, 15c, 15e und 15g, 22, 25a und 25b entstehen.
Heterocyclen via Mannichbasen, 7. Mitt. Synthese von Pyrazolo[1,5‐a]pyrido[2,3‐d]pyrimidin‐9(4H)‐onen
Authors: Klein Hans Jürgen , Troschütz Reinhard , Roth Hermann J.
Published: October 2006

Die Titelverbindungen 4 lassen sich aus 5‐Amino‐3‐methylpyrazolo[1,5‐a]pyrid‐7(4H)‐on (2) und Keton‐Mannichbasen oder Dehydro‐Keton‐Mannichbasen darstellen.
Herbizide, 3. Mitt. Synthese von 4,6‐Dialkyl‐2‐cyanaminopyrimidinen und Untersuchungen ihrer Struktur durch 13C‐NMR‐Spektroskopie
Authors: Kreutzberger Alfred , Sellheim Michael
Published: October 2006

Die Kondensation von Dicyandiamid (1) mit den β‐Diketonen 2a–c führt zu den 2,4‐unsymmetrisch substituierten 2‐Cyanaminopyrimidinen 3a–c, für deren Struktur sich aus den13C‐NMR‐spektroskopischen Untersuchungen das Vorliegen eines Gleichgewichts mit den tautomeren Formen 7 und 8 der 2‐Cyaniminopyrimidine ableitet. Das 2‐Cyanamino‐4,6‐diethylpyrimidin hat sich als herbizid wirksam erwiesen.
Chirale 3‐Aminopropanole, 1. Mitt. Synthese der Racemate und der Enantiomere
Authors: Knabe Joachim , Buchheit Wolfgang
Published: October 2006

Ausgehend von racem. und optisch aktiven disubstituierten Cyanessigestern wurden die 3‐Aminopropanole 5a–5d hergestellt. Dabei erwies sich die Reduktion der Cyanessigester in 2 Stufen als erfolgreicher als die direkte Umsetzung mit LiAlH4. Zunächst wurde die Nitrilgruppe katalytisch zur Aminogruppe hydriert, dann mit LiAlH4 die Esterfunktion reduziert. Die racem. und optisch aktiven cyclohexylsubstituierten 3‐Aminopropanole 5e und 5f wurden durch Hydrierung von 5c und 5d mit Pd/C erhalten. Die absolute Konfiguration der optisch aktiven 3‐Aminopropanole wurde aus der der Ausgangsverbindungen abgeleitet.
Chemical Properties‐Dissolution Relationship of Non‐Steroidal Antiinflammatory Acidic Drugs, I. Release of Naproxen from Inert Matrices
Authors: Zecchi Vittorio , Tartarini Annarosa , Conte Ubaldo , Fini Adamo
Published: October 2006

The dissolution of naproxen from inert matrices (monoliths) has been studied; the matrices were obtained by direct compression using polymeric materials as support. The influence of the chemical form employed (acid or salt) and of the affinity of the drug to the supporting material on the release process are discussed. Release experiments were carried out in the columnar cell of a laminar flux apparatus. They showed that the solubility of the chemical form employed is more important for the dissolution of naproxen from monoliths than the drug's affinity to the supporting material.
1,2,3,4‐Tetrahydrophthalazine, 3. Mitt. 2,4‐Dialkyl‐2,3,4,5,7,12‐hexahydro‐1H‐(1,2,5)triazepin[1,2‐b]phthalazin‐1,5‐dione
Authors: Groszkowski Stefan , Wesołowska Barbara , Wrona Jadwiga
Published: October 2006

Durch Kondensation von 2,3‐Bis‐(2‐bromacyl)‐1,2,3,4‐tetrahydrophthalazinen mit primären Aminen wurde eine Reihe von 3‐substituierten 2,4‐Dialkyl‐2,3,4,5,7,12‐hexahydro‐1H‐(1,2,5)triazepin[1,2‐b]phthalazin‐1,5‐dionen erhalten.
Zur Umsetzung von Aminen mit Phthalaldehyd, 2. Mitt. Röntgenstrukturanalyse von 3‐Chlor‐5‐phenyl‐5,11‐dihydroisoindolo‐[2,1‐a] chinazolin
Authors: Troschütz Jutta , Kirfel Armin , Will Georg
Published: October 2006

Durch Röntgenstrukturanalyse wird für das Cyclokondensationsprodukt aus Phthalaldehyd und 2‐Amino‐5‐chlorbenzhydrylamin aus saurer Lösung die Struktur eines Dihydroisoindolo[2,1‐a]chinazolins bewiesen.
Lactone, 6. Mitt. H1‐Histaminolytische, neurotrop spasmolytische und zentral sedierende α‐Aminomethyl‐γ,γ‐diaryl‐γ‐lactone
Authors: Lehmann Jochen , Gajewski Gisela , Wolf Gerd
Published: October 2006

γ‐Aryl‐ und γ,γ‐Diarylbutyrolactone werden durch Formylierung und anschließende reduktive Aminoalkylierung in Verbindungen überführt, die man als lactonverbrückte Aryl‐ 7 bzw. Diaryl‐alkylamine 8,9 betrachten kann. Einige dieser Substanzen wurden auf H1‐histaminolytische, neurotrop spasmolytische und zentrale Wirkung geprüft. Das Spirolacton 9a besitzt die maximale, dem Atropinsulfat überlegene spasmolytische Wirkung, aber keine antipsychotische Aktivität. Die Aminomethyl‐diaryllactone 8 wirken histaminolytisch, spasmolytisch und schwach bis mäßig zentral sedierend.
Eine einfache Synthese von γ‐Sultinen
Authors: Messinger Paul
Published: October 2006

A Convenient Synthesis of γ‐Sultines
Stereochemie substituierter Glutarsäuren, 1. Mitt. (±)‐threo‐ und erythro‐2‐Methyl‐3‐phenylglutarsäuren
Authors: Frahm August W.
Published: October 2006

Es wird die Reindarstellung und Konfigurationszuordnung der (±)‐threo‐ und erythro‐2‐Methyl‐3‐phenyl‐glutarsäuren (5, 6) über die (±)‐threo‐ und erythro‐2‐Phenylbutan‐1.1.3‐tricarbonsäuren (3, 4) beschrieben.
Cyclotrimerisierung von 1‐Phenyl‐2‐propin‐1‐ol
Authors: Möhrle Hans , Platzek Thomas
Published: October 2006

Die Umsetzung on 1‐Phenyl‐2‐propin‐1‐ol in NaH/DMSO führt in Gegenwart von Pyrrolidin‐2‐on zu einem Gemisch von 1,3,5‐ und 1,2,4‐Tribenzoylcyclohexan. Weiteren Reaktionen und spektroskopische Eigenschaften werden beschrieben.
Untersuchungen an 1,3‐Thiazinen, 28. Mitt. Reaktionen von 3‐Amino‐2‐thioxo‐tetrahydro‐(4H)‐1,3‐thiazin‐4‐onen mit Nucleophilen
Authors: Hanefeld Wolfgang , Staude Hans‐Jürgen
Published: October 2006

3‐Amino‐2‐thioxo‐tetrahydro‐(4H)‐1,3‐thiazin‐4‐one 1 werden durch Nucleophile bevorzugt an der N‐3‐C‐4‐Bindung gespalten. Mit einigen Stickstoffbasen erfolgt unter verschärften Bedingungen zusätzlich Spaltung der S‐1‐C‐2‐Bindung zu Thiosemicarbaziden.
Synthese von 7‐Amino‐norkhellin‐6‐carbonitrilen
Authors: Eiden Fritz , Schünemann Jürgen
Published: October 2006

Die 7‐Amino‐norkhellin‐6‐carbonitrile 13a–13c lassen sich aus dem entsprechenden 7‐Methylthio‐Derivat 11 gewinnen, das durch Reaktion des Acyl‐acetonitrils 9 mit CS2/KOH/DMS entsteht; daneben wurde das Thiopyrano‐benzofuran‐Derivat 12 isoliert, das sich zu den aminsubstituierten Carbonitrilen 14a–14c umsetzen läßt.
Intramolekulare Aromatenalkylierungen, 16. Mitt. Synthese von 4‐Methyl‐ und 2,4‐Dimethyl‐5‐benzyl‐5,6,7,8‐tetrahydrochinolinen
Authors: Reimann Eberhard , Friesinger Josef M.
Published: October 2006

Aus den Methylchinolinonen 6, 7 und den Grignard‐Reagenzien 8 werden glatt die tertiären Carbinole 9, 10 erhalten. Eine Substitution in 2‐Stellung des Heterocyclus ist nur bei der Reaktion von 6 und 8c nachweisbar, wobei neben 9c das 2‐Benzylchinolinon 13 entsteht. Durch kombinierte Dehydratisierung/Hydrierung lassen sich die Carbinole 9, 10 bequem in die Titelverbindungen 11, 12 umwandeln. Die Verknüpfung der Chinolinone 6, 7 mit einem Benzylrest durch Carbonylolefinierung gelingt nicht.
Potentielle Radiopharmaka zur Nebennierenszintigraphie, 3. Mitt. Tierexperimentelle Studien mit 131Iod markierten Tyraminyl‐ und p‐Hydroxyphenyl‐Aglyka
Authors: Röder Erhard , Lütz Johannes , Biersack Hans‐Jürgen , Winkler Cuno
Published: October 2006

Von 6 Verbindungen wird die Organverteilung an Wistar‐Albinoratten ermittelt. Mit 131I‐3‐Tyraminyl‐3‐desoxy‐dihydrodigitoxigenin (1) und 131I‐3‐Tyraminyl‐3‐desoxy‐scillarenin (2) lassen sich die Nebennieren schon nach 2h darstellen. Von 1 werden Szintigramme von Hunden aufgenommen, wobei die an Ratten erzielten Ergebnisse bestätigt werden.
Zur Stereochemie der 3‐Oxo‐5‐phenyl‐1‐cyclopentancarbonsäuren, 8. Mitt. Synthese kernfluorierter, stereomerer 5‐Phenyl‐dihydrosarkomycine, Teil 2
Authors: Körfer Inge , Frahm August W.
Published: October 2006

Es wird die stereoselektive Synthese der drei 5‐(4‐Fluorphenyl)‐dihydrosarkomycine 3–5 aus trans‐4‐Fluorzimtsäuremethylester und Propan‐1.1.2‐tricarbonsäuretrimethylester über die Dieckmannringschlußprodukte 1 und 2 beschrieben.
Arzneimittelanalysen mittels polarographischer Methoden, 26. Mitt. Polarographische Bestimmung (DPP) des Lepra‐Therapeutikums Diaphenylsulfon (Dapsone)
Authors: Oelschläger Herbert , Modrack Gotelinde
Published: October 2006

Diaphenylsulfon (1) wird an der Hg‐Tropfelektrode (DME) in CH3CN (TEAI als Leitelektrolyt) unter Verbrauch von 2 Elektronen reduziert. Der DPP‐Peak ist nach Zugabe von 3 % Wasser als Protonendonator besser auswertbar als die DCP‐Kurve. Der Gehalt von 1 in den D.A.D.P.S.‐Tabletten (Bayer AG, Leverkusen) kann polarographisch mit einer srel = ± 2,46 % schnell bestimmt werden.
Antiphlogistische 2.3‐Dihydro‐1H‐pyrrolizine, 3. Mitt. Aminomethylierung und Arylthiolierung von 6.7‐Diaryl‐2.3‐dihydro‐1H‐pyrrolizinen
Authors: Dannhardt Gerd , Steindl Ludwig
Published: October 2006

6.7‐Diaryl‐2.3‐dihydro‐1H‐pyrrolizine (DADHP) werden durch SE‐Reaktion en C‐5 zu Aminomethyl‐ 1 und Arylthioderivaten 3 funktionalisiert. Die Pyrrolizinylthioether 3 besitzen starke antiphlogistische Wirksamkeit, die bei den Aminomethylverbindungen nur wenig ausgeprägt ist.
Reaction of Uric Acid with 2,6‐Dichloroquinone‐4‐chlorimine
Authors: Kovar Karl‐Artur , Teutsch Michael
Published: October 2006

Harnsäure setzt sich mit 2,6‐Dichlorchinon‐4‐chlorimin (DCI) in alkalischer Lösung zu einem gelben Farbstoff um, der in Kombination mit einer enzymatischen Reaktion zur quantitativen Bestimmung in Harn und Serum herangezogen werden Kann2). In der Literatur existieren verschiedene Angaben über die NH‐Aciditäten der Harnsäure, so daß die Kupplungsstelle mit DCI strittig ist: Danach müßte das Reagens entweder an N‐93) oder an N‐34) angreifen. Fearon6) hatte dagegen die Substitution der Harnsäure an N‐7 angenommen, konnte aber dieses Postulat experimentell nicht überprüfen, da ihm die Isolierung des Umsetzungsproduktes mißlang. Zur Klärung der Verhältnisse wurde der Farbstoff aus Harnsäure [7‐15N] und DCI hergestellt und NMR‐spektroskopisch vermessen.
H2‐Antihistaminika, 31. Mitt.1). 1,2,5‐Triazin‐2,4‐diamine und ‐2,4,6‐triamine mit H2‐antagonistischer Wirkung
Authors: Mohr Rainer , Buschauer Armin , Schunack Walter
Published: October 2006

Es wurden N‐[3‐(3‐piperidinomethyl‐phenoxy)propyl]‐substituierte 6‐Alkoxy‐1,3,5‐triazin‐2,4‐diamine und 1,3,5‐Triazin‐2,4,6‐triamine dargestellt und am isolierten Meerschweinchenvorhof sowie zum Teil an der histaminstimulierten Säuresekretion der narkotisierten Ratte auf H2‐antagonistische Wirkung untersucht.
Monosulfonyl‐cyclopentadiene
Authors: Hartke Klaus , Jung Myung Hee , Zerbe Horst , Kämpchen Thomas
Published: October 2006

Die Addition von Sulfonsäurebromiden an Cyclopentadien (1) liefert ein Gemisch der cis‐ und trans‐3‐Brom‐5‐sulfonylcyclopentene 7 und 8, deren Sterochemie sowohl 1H‐NMR‐spektroskopisch als auch durch gezielte Abwandlungsreaktionen geklärt wird. Mit Natriumhydrid erhält man aus 7 oder 8 die Natriumsulfonylcyclopentadienide 15, die sich durch Austausch des Kations in die stabileren Salze 16 überführen lassen. Die aus 15 oder 16 durch Säure gebildeten Monosulfonylcyclopentadiene 17 sind sehr instabil und gehen sofort in die Diels‐Alder‐Dimere 6 über. Dabei konnte nur das 1‐Phenylsulfonyl‐cyclopentadien (17a) abgefangen und näher charakterisiert werden.
Zur Stereoselektivität der Reduktion phenylsubstituierte γ‐Aminoketone
Authors: Graßhoff Lutz , Haller Rolf
Published: October 2006

Bei der Reduktion phenylsubstituierter γ‐Aminoketone mit Natrium/Propanol oder mit Lithium‐aluminiumhydrid werden unterschiedlich zusammengesetzte Diastereomerengemische erhalten. Die Diastereoselektivität dieser Reduktionen läßt sich mit den von Chérest und Mitarb. vorgeschlagenen Modellvorstellungen gut vereinbaren.
Sex difference in diffuse malignant peritoneal mesothelioma
Authors: Yan T D , Popa E , Brun E A , Cerruto C A , Sugarbaker P H
Published: October 2006

Background

Diffuse malignant peritoneal mesothelioma (DMPM) is rare and in the past has proved an invariably fatal disease. Female patients have been reported to have an improved survival outcome for reasons that are not understood.

Methods

The survival of 34 men and 28 women who underwent cytoreduction and perioperative intraperitoneal chemotherapy for DMPM was compared. Twenty-five clinicopathological variables were subjected to univariate analysis.

Results

The women had a 5-year survival rate of 63 per cent and median survival was not reached. The men had a 5-year survival rate of 42 per cent, with a median survival of 32 months (P = 0·045). Women had undergone more extensive previous surgery and had less extensive peritoneal involvement at the time of cytoreduction. Tumours in women more frequently showed a small nuclear size (30 µm or less) and the chromatin pattern was more often granular than clear.

Conclusion

Women with DMPM had better survival. This observation may be related to the favourable clinical and histopathological features associated with women.
Improved operative and survival outcomes of surgical treatment for hilar cholangiocarcinoma
Authors: Liu C L , Fan S T , Lo C M , Tso W K , Lam C M , Wong J
Published: October 2006

Background

The aim of the present study was to assess whether an aggressive surgical approach in the management of patients with hilar cholangiocarcinoma was associated with improved operative and survival outcomes.

Methods

Eighty-two patients with hilar cholangiocarcinoma treated between 1989 and 1998 (period 1), and 60 patients treated between 1999 and 2004 (period 2), were evaluated. Modifications to management in period 2 primarily included percutaneous biliary drainage instead of endoscopic drainage for relief of obstructive jaundice, preoperative right portal vein embolization before right-sided hepatectomy, routine total caudate lobectomy and radical lymphadenectomy during surgical resection of the tumour.

Results

The surgical resection rate was significantly higher in period 2 than in period 1 (45 versus 16 per cent; P < 0·001). All patients in period 2 underwent major hepatectomy with concomitant caudate lobectomy. The operative morbidity and hospital mortality rates decreased significantly in period 2 compared with period 1, with significantly better survival outcomes. In multivariate analysis, resection of the tumour in period 2 and operative blood loss of 1·5 litres or less were the significant independent factors associated with improved survival.

Conclusion

An aggressive surgical approach was associated with improved operative and survival outcomes for patients with hilar cholangiocarcinoma.