bluuebunny/crossref_metadata_2025_split huggingface dataset:
Electron Impact Induced Loss of C‐5/C‐8 Substituents of 1,2,3,4‐Tetrahydroisoquinolines, VI1): Synthesis and Mass Spectrometric Fragmentation of Dihydroindole Derivatives
Authors: Knefeli Frank , Mayer Klaus K. , Wiegrebe W. , Schlunegger Urs P. , Lauber Rolf 
Published: October 2006

AbstractThe syntheses of the C‐4 substituted dihydroindoles 25, 31 (scheme 7), and 36 (scheme 8) are described. ‐ The CID MIKE spectrum in the 2. field free region (2. FFR) of m/z 146 from 25 is very similar to but not identical with that of m/z 146 from the C‐5 substituted tetrahydroisoquinolines 3, 6, 7, and 8 (scheme 2), so supporting our hypothesis of a rearrangement in M+ of tetrahydroisoquinolines1) prior to fragmentation, but not proving it. As the CID MIKE spectra of the tetrahydroisoquinolines 3, 6, 7, and 8 are not identical among each other we assume that a 1.3‐H‐shift takes places in their M+ in competition to the rearrangement mentioned above.
Quantitative Struktur‐Wirkungs‐Beziehung bei Polyhydroxyxanthonen, 2. Mitt.1): Synthese mehrfach oxigenierter 2‐Hydroxyxanthone
Authors: Mahfouz Nadia M. A. , Hambloch Heinrich , Omar Nabil M. , Frahm August W. 
Published: October 2006

AbstractEs wird die Synthese der 2‐Hydroxyxanthone 8 über die entsprechenden Polymethoxyxanthone 7 beschrieben, die in Ring C mehrfach hydroxyliert sind. Die Darstellung verläuft entweder über die 2‐Phenoxybenzosäuren 5 oder die polymethoxylierten 2‐Hydroxybenzophenone 6.
Researches on Antibacterial and Antifungal Agents, XII1): Analogues of Bifonazole with Two Imidazole Moieties and Related Azoles
Authors: Stefancich Giorgio , Silvestri Romano , Panico Salvatore , Artico Marco , Simonetti Nicola 
Published: October 2006

AbstractAnalogues of bifonazole bearing two imidazole rings and other related azoles have been synthesized and tested as antifungal agents against Candida albicans and Candida spp., Only a slight part of the antifungal power of the parent drug is retained by some derivatives as evinced by the comparison of new compounds with bifonazole, miconazole, and ketoconazole.
Tumor Inhibiting [1,2‐Bis(fluorophenyl)ethylenediamine]platinum(II) Complexes, III1): Evaluation of the Mammary Tumor Inhibiting Properties
Authors: Reile Herta , Spruß Thilo , Müller Richard , Gust Ronald , Bernhardt Günther , Schönenberger Helmut , Engel Jürgen 
Published: October 2006

AbstractDiastereomeric diaqua[1,2‐bis(4‐fluorophenyl)ethylenediamine]platinum(II) sulfates and nitrates produce a strong inhibition of the hormone‐dependent MXT‐M 3.2 mammary carcinoma of the B6D2F1 mouse. Besides an interference in the DNA synthesis in analogy to cisplatin a lowering of the estrogen level due to an interference in steroid biosynthesis is suggested as the mode of action. In contrast to the R,R/S,S configurated diaqua[1,2‐bis(4‐fluorophenyl)ethylenediamine]platinum(II) salts the corresponding R,S configurated compounds are also markedly active on the hormone‐independent MXT‐Ovex mammary carcinoma of the B6D2F1 mouse.
Measurement of Carvedilol Enantiomers in Human Plasma and Urine Using S‐Naproxen Chloride for Chiral Derivatization
Authors: Spahn Hildegard , Henke Werner , Langguth Peter , Schloos Jürgen , Mutschler Ernst 
Published: October 2006

AbstractThe enantiospecific procedure for assaying carvedilol includes the extraction of the drug from plasma or urine with diisopropylether after alkalization of the sample with pH 9.8 buffer. After evaporation of the org. solvent a chiral derivatization is performed using S‐(+)‐naproxen chloride. The HPLC separation of the diastereomeric amides is possible on a silica gel stationary phase with a mixture of n‐hexane, dichloromethane, and ethanol as mobile phase. Detection of the products is performed by fluorescence measurement at 285/355 nm.Preliminary pharmacokinetic studies after i.v. infusion of racemic compound to healthy volunteers showed that the concentrations of the R‐(+)‐enantiomer exceeded those of the S‐(−)‐enantiomer. Overall, both carvedilol enantiomers exhibited a high clearance with preference for the S‐enantiomer. The difference was even more expressed after p.o. dosage indicating a stereoselective first‐pass effect with higher extraction of the levorotatory enantiomer, which is more potent with respect to β‐adrenoceptor antagonistic activity.
Hypertensiv wirksame 5‐(ω‐Aminoalkyl)aminoisoxazole: Synthese und Prüfung von Verbindungen mit einer Sulfamid‐ oder Carboxyl‐Gruppe am Ende der Seitenkette
Authors: Dannhardt Gerd , Dominiak Peter , Laufer Stefan 
Published: October 2006

Abstract5‐(ω‐Aminoalkyl)aminoisoxazoles with Hypertensive Activity: Synthesis and Screening of Compounds with a Sulfamide or Carboxyl Function at the End of the Side Chain
2‐Amino‐2‐oxazolines, II: Reactivity of the Nitrogens. Crystal Structures of Two endo/exo N‐Substituted Compounds
Authors: Bosc Jean‐Jacques , Forfar Isabelle , Jarry Christian , Ouhabi Jamal , Leger Jean‐Michel , Carpy Alain 
Published: October 2006

AbstractThe amidine group of the five‐membered heterocycle induces a tautomeric amino/imino equilibrium. In the 2‐amino‐2‐oxazoline form the endo nitrogen is more reactive than the exo one. In the imino‐2‐oxazolidine form, the contrary occurs. Depending on the experimental conditions, substitutive reactions take place either on the endo or on the exo nitrogen. The crystal structures of two endo/exo N‐substituted compounds were determined by X‐ray crystallography.
Hypolipidemic Activity in Rodents of Phenobarbital and Related Derivatives
Authors: Hall I. H. , Patrick M. A. , Maguire J. H. 
Published: October 2006

AbstractA series of 5‐alkyl‐5‐phenylbarbituric acid analogues were shown to be potent hypolipidemic agents in rats and mice at 20 mg/kg/day. This dose is tower than that required for hypolipidemic activity for clofibrate and nicotinic acid derivatives in rodents and man. These new derivatives reduced both serum cholesterol and triglyceride levels in rodents by either the oral or intraperitoneal route of administration. Previous studies have demonstrated that similar heterocyclic compounds, i.e. cyclic imides, glutarimides and hydantoins are potent hypolipidemic agents in rodents. The barbituric acid derivatives probably interfered with de novo synthesis of cholesterol and fatty acids in the early steps since the agents inhibit the activities of ATP‐dependent citrate lyase and acetyl‐CoA synthetase. Triglyceride synthesis may be blocked since the agents inhibited the rate limiting enzyme, sn‐glycerol‐3‐phosphate‐acyl‐transferase. Rat tissue lipids especially cholesterol and triglycerides were reduced after 14 days treatment. Fecal lipids were increased in cholesterol and phospholipid content by selected compounds. The rat serum lipoprotein after 14 days drug administration showed reduced VLDL‐cholesterol and chylomicron‐cholesterol content with elevated HDL‐cholesterol and HDL‐triglyceride contents. The modulation of the lipid content of the serum lipoproteins by the barbituric acids suggest that these agents may be helpful in treating clinical hyperlipidemic disease states.
Synthesis and Antimicrobial Activities of Some New Tetrahydro‐2H‐1,3,5‐thiadiazine‐2‐thione Derivatives of Ampicillin
Authors: Ertan Mevlüt , Tayhan Ayla Balkan , Yulug Nuran 
Published: October 2006

AbstractCompounds having α‐[dihydro‐5‐substituted 6‐thioxo‐ 2H‐1,3,5‐thiadiazine‐3(4H)‐yl]benzylpenicillin structure were synthesized by the reaction of ampicillin trihydrate, formaldehyde and dithiocarbamic acid salts. The structures were evident from chemical and spectral analysis. The antimicrobial activities of the compounds were investigated against some gram‐positive (Staphylococcus aureus and Streptococcus faecalis) and gram‐negative (Escherichia coli and Pseudomonas aeruginosa) bacteria and some yeast‐like fungi (Candida albicans, C. parapsilosis, C. stellatoidea and C. pseudotropicalis) and molds such as Trichophyton rubrum, T. mentagrophytes, Microsporum canis, M. gypseum, Penicillium and Aspergillus by the tube dilution method. In addition to MIC (minimal inhibitory concentration), MBC (minimal bactericidal concentration) and MFC (minimal fungicidal concentration) values were determined using ampicillin trihydrate as standard. The compounds synthesized were usually found as effective as ampicillin trihydrate against S. aureus and S. faecalis and less effective than ampicillin trihydrate against E. coli. Both the compounds synthesized and ampicillin trihydrate are ineffective in the concentrations studied against P. aeruginosa. Compound 10 and 11 are more effective against all the yeast‐like fungi than the other compounds and ampicillin trihydrate.
Quinazolinones, XVII1): Synthesis and Pharmacological Activities of Some Antipyryloxoalkylthioquinazolinones
Authors: Gürsoy Aysel , Büyüktimkin Servet , Demirayak Seref , Ekinci Ahmet C. 
Published: October 2006

AbstractChinazolinone, 17. Mitt.1): Synthese und pharmakologische Wirksamkeit einiger Antipyryloxoalkylthiochinazolinone
Intramolekulare Aminoalkylierung von Amidoximen
Authors: Möhrle Hans , Lessel Jürgen 
Published: October 2006

Abstract2‐tertiär‐Amino‐benzamidoxime 2 erfahren bei der Umsetzung mit dem Quecksilber(II)‐EDTA‐Komplex eine intramolekulare Aminoalkylierung und Oxidation zu anellierten Chinazolinon‐oximen 5, wobei die Konfiguration erhalten bleibt.
5‐[(Halo)fluoralkyl]‐5‐hydroxyimidazolidin‐2,4‐dione aus 2,4,5‐Imidazolidintrionen
Authors: Broicher Volker , Geffken Detlef 
Published: October 2006

AbstractDie (Halo)fluoralkyltrimethylsilane 2 reagieren leicht mit den Imidazolidintrionen 1 in Gegenwart von Tetrabutylammoniumfluorid (TBAF) zu den 5‐[(Halo)fluoralkyl]‐5‐hydroxyimidazolidin‐2,4‐dionen 4.
Synthesis of N‐Substituted 3′‐Amino‐3′‐deoxythymidines and their Biological Evaluation against HIV
Authors: Motawia Mohammed S. , Pedersen Erik B. , Nielsen Carsten M. 
Published: October 2006

AbstractTreatment of 3′‐amino‐3′‐deoxythymidine (1) with carboxylic acid anhydrides afforded the corresponding acylamino derivatives 2a–f. Reaction of 1 with a variety of isothiocyanates led to the corresponding thioureido derivatives 3a–i. Also, conversion of 1 into 3′‐carbylamino‐3′‐deoxythymidine (7) is reported. The compounds 2, 3, and 8 were evaluated for their anti‐HIV activity in MT‐4 cells, but did not show sufficient efficacy.
Antineoplastika, 19. Mitt.: Darstellung von N‐[2‐Chlor‐4‐diethylamino‐(1,3,5‐triazin‐6‐yl)]‐aminosäuren
Authors: Kreutzberger Alfred , Langner Peter , Stratmann Jörg 
Published: October 2006

AbstractPreparation on N‐[2‐Chloro‐4‐diethylamino‐1,3,5‐triazin‐6‐yl)]‐amino Acids
Pharmakokinetik von Carboplatin nach intraperitonealer Verabreichung
Authors: Czejka Martin , Jäger Walter , Schüller Johann , Teherani Davoud 
Published: October 2006

AbstractDer Konzentrationsverlauf des Krebschemotherapeutikums Carboplatin wurde im Serum und in der Intraperitonealflüssigkeit (IPF) von sechs Patientinnen bestimmt. Die pharmakokinetische Auswertung zeigte eine rasche Verteilungsphase innerhalb der ersten 4 h nach Infusionsbeginn zwischen beiden Kompartimenten (t1/2 Serum = 4.4 h, t1/2 IPF = 3.3 h). Die terminale Elimination von Carboplatin aus dem Blutgefäßsystem lag mit t1/2 el = 20.3 h deutlich höher als aus der IPF (t1/2 el = 10.6 h). Die Verfügbarkeit (berechnet als AUC‐Werte) lag innerhalb von 48 h für die Intraperitonealflüssigkeit zumindest 6 mal höher als für das Serum, wobei 98 % der bestimmten Menge während dieser Zeit aus beiden Kompartimenten eliminiert wurden. Die erwünscht hohen IPF‐Spiegel sprechen für diese Verabreichungsform.
Spectrofluorimetric Assay of Fluoride Ions in Pharmaceutical Formulations
Authors: Raggi M. A. 
Published: October 2006

AbstractFluorides, already well known for their toxic properties, have been the subject of a renewed interest as therapeutic agents in recent years. Their beneficial effects e.g. in preventing dental caries and vertebral osteoporosis1,2) have resulted in a number of commercial formulations. The toxicity of the fluoride ion is, however, rather pronounced; it inhibits a number of enzymatic systems and reduces tissue respiration and anaerobic glycolysis3); prolonged treatment can lead to osteosclerosis and to the calcification of soft tissue adhering to the bones. Consequently, especially in long terms treatments, very low dosage forms, from 0.001 g (adults) to 0.00025 g (children) of fluoride have to be employed: the monitoring of this ion in organic fluids as well as its accurate determination in pharmaceutical formulations has to be therefore continuously upgraded. The titration in non aqueous solvent, reccomended by a few pharmacopoeias4‐6), with perchloric acid as titrant and crystal violet as indicator, is lacking sensitivity. Other more sensitive methods are reported and they include the potentiometric analysis of F by means of a LaF3 membrane electrode7) and the spectrophotometric assay based on the use of Zr‐Alyzarine8) or Ce‐Alyzarine complex9); unfortunately they are not free from interferences8).In the present note we propose as an alternative to the above methods, a simple and selective spectrofluorimetric procedure.
Synthese von Pyrrolizincarbonsäureaniliden durch 1,3‐Cycloaddition von Prolin mit Acetylenen und nachfolgende Reaktion zu Carbonsäureaniliden
Authors: Röder Erhard , Kupferberg Ralf 
Published: October 2006

AbstractUmsetzungen von Prolin mit Acetylencarbonsäurederivaten in Acetanhydrid führen durch 1,3‐Cycloaddition über mesoionische Oxazolonzwischenstufen zu Pyrrolizincarbonsäureester. Diese werden mittels einer Stickstoff‐Grignardierung zu den entspr. Aniliden umgesetzt. Die Strukturen werden durch spektroskopische Daten belegt.
Synthesis and Biological Evaluation of 14‐Alkoxymorphinans, V1): 6‐Deoxocyprodime, an Opioid Antagonist with Decreased μ Receptor Selectivity in Comparison to Cyprodime
Authors: Schmidhammer Helmut , Jennewein Herwig K. , Smith Colin F. C. 
Published: October 2006

AbstractN‐Cyclopropylmethyl‐4,14‐dimethoxymorphinan (4) and N‐cyclopropylmethyl‐4‐hydroxy‐14‐methoxymorphinan (5) have been prepared from cyprodime (1) by Wolff‐Kishner reduction. Pharmacological studies (mouse vas deferens and guinea pig ileum preparations) revealed that there was no significant decrease of 4 in antagonist activity but in μ selectivity when compared with 1. The phenol 5 showed partial agonism at μ, κ and δ receptors.
Potentielle Antiöstrogene vom Typ des 1,2‐Diphenyl‐1‐pyridyl‐but‐1‐ens. Teil 2: Biologische Prüfung
Authors: Schwarz Walter , Hartmann Rolf W. , Schönenberger Helmut 
Published: October 2006

AbstractDie Z‐1‐(4‐Hydroxyphenyl)‐1‐(4‐bzw. 3‐pyridyl)‐2‐phenyl‐but‐1‐ene Z‐1 und Z‐2 und ihre Acetate Z‐1a und Z‐2a sind schwache Östrogene (Uterusgewichtstest, juvenile Maus), die am hormonabhängigen MXT‐Mammacarcidom der Maus eine ausgeprägte Hemmung des Tumorwachstums hervorrufen. Östrogene Nebenwirkungen (Uterusgewichte) treten im Tumorversuch nicht oder nur in geringem Ausmaß auf.
Platelet Aggregation Inhibiting and Anticoagulant Effects of Oligoamines, XIV: Branched Aliphatic and Alicyclic Triamines and Tetramines
Authors: Rehse Klaus , Kesselhut Andreas , Schein Volkmar , Leißring Susanne 
Published: October 2006

AbstractTwenty‐four triamines and three tetramines were synthesized. Seventeen triamines inhibited platelet aggregation induced by collagen at a concentration below 10 μmol/L (IC50). Ten triamines in a 100 μmolar concentration inhibited fibrin formation induced by thromboplastin by more then 75 %. Both effects do not run parallel. They are strongly dependent from the steric and lipophilic properties of the title oligoamines. The tetramines were nearly inactive.
Synthesis and Antifungal Activity of Some New Benzimidazole Derivatives
Authors: Göker Hakan , Ertan Rahmiye , Akgün Hülya , Yulug Nuran 
Published: October 2006

AbstractSynthesis and antifungal evaluation of 5‐ethoxycarbonyl‐2‐(substituted‐benzyl or phenoxymethyl)benzimidazoles are reported. Structures of the compounds were elucidated with IR‐, 1H‐NMR‐, 13C‐NMR‐, mass‐spectra and elemental analysis. Preliminary results show that none of the synthesized benzimidazole derivatives has antifungal activity at the concentration of 100 μg/ml against Candida parapsilosis, Candida stellatoidea, and Candida pseudotropicalis.
Platelet Aggregation Inhibiting and Anticoagulant Effects of Oligoamines, XV: Antithrombotic Effect of Selected Oligoamines in Rats
Authors: Rehse Klaus , Kesselhut Andreas , Schein Volkmar , Kämpfe Michael , Rose Bettina , Unsöld Eberhard 
Published: October 2006

AbstractOligoamines which exert antiplatelet and anticoagulant properties in vitro show as well antithrombotic effects in mesenteric arterioles and venoles of rats. The formation of thrombi in these vessels was induced by a laser beam and quantified by the thrombus formation index (TFI). The most potent compound RE 1492 already reduced the formation of thrombi after i.v. administration of 1 mg/kg significantly. After oral administration, however, only a minor effect even after a 200 mg/kg dose is observed. This suggests that the oligoamine was poorly absorbed from the gastrointestinal tract. The tricarbamate of RE 1492 ( RE 1492 C), however, was a suitable prodrug. Eight hours after a single oral dose of 10 mg/kg significant antithrombotic properties in arterioles and venoles were seen, (TFI = 3.63 (A), 1.77 (V); control: 1.76 (A), 1.29 (V).) After p.o. application of 30 mg/kg RE 1492 C the onset of activity is after 2 h (TFI = 3.44/1.48). A maximum effect is reached after 4 h (TFI: 4.43/2.84) and maintained up to 24 h (TFI = 4.49/2.45). After 48 h the effect in arterioles is still significant (p < 0.05, χ2‐test). The results obtained with five other carbamates (RE 2029 C, RE 1964 C, RE 2120 C, RE 2112 C, and RE 1981 C) 4 h after p.o. administration in general show a stronger effect in arterioles than in venoles which is in the same range as in RE 1492 C.
Quecksilber(II)‐EDTA‐Dehydrierung N‐ und O‐funktionalisierter 2‐tert‐Amino‐benzamidoxime
Authors: Möhrle Hans , Lessel Jürgen 
Published: October 2006

AbstractDie O‐ bzw. N‐/O‐Acylierung des 2‐Piperidinobenzamidoxims bewirkt eine Modifizierung des Reaktionsverhaltens unter den Bedingungen der Quecksilber(II)‐EDTA‐Dehydrierung; Hydrolyse und Acylwanderung treten in Konkurrenz mit der intramolekularen Aminoalkylierung.
Intramolekulare Iminium‐Sulfonylharnstoff‐Reaktionen
Authors: Möhrle Hans , Niefenthaler Hans 
Published: October 2006

Abstract2‐Amino‐5‐nitrobenzosulfonylharnstoffe 10—12 geben bei der Dehydrierung mit Natriumquecksilberedetat unter Verlust des Carbamoyl‐Anteils über die Zwischenstufe der Sulfonylaminale 4—6 die Sulfonylamidine 7—9. ‐ Beim entspr. Pipecolin‐Derivat 18 führt die Oxidation unter Entcarbamoylierung und Ringöffnung zum Aminoketon 16.
Reaktionen von Monosulfonyl‐cyclopentadieniden
Authors: Hartke Klaus , Lee Myung‐Hee 
Published: October 2006

AbstractDie elektrophile Substitution der Monosulfonyl‐cyclopentadienide 4 mit Dimethylsulfoxid/Trifluoracetanhydrid oder Dimethylsulfid/N‐Chlorsuccinimid liefert ein Gemisch der 1,2‐ und 1,3‐Bissulfoniocyclopentadienide 5 und 6. Mit 4 und Tetrahydrothiophensulfoxid (7)/Trifluoracetanhydrid erhält man bei −40°C ebenfalls ein Gemisch von 5 und 6, bei −10°C jedoch die Trissulfonio‐cyclopentadienide 8. N,N,S‐Trimethyl‐thioformininium‐iodid (9) kondensiert mit 4 zu einem Gemisch der heterosubstituierten Fulvene 10 und 11.
Synthesis and Anticonvulsant Properties of Some Novel Quinazolone‐thiosemicarbazone and 4‐Thiazolidone Derivatives
Authors: El‐Feky S. A. H. , Abd El‐Samii Z. K. 
Published: October 2006

AbstractDiverse biological activities have been found in compounds having a quinazolinone ring system1). A large number of 4(3H)‐quinazolinones, in particular those possessing 2‐alkyl‐3‐aryl2), 2,3‐dialkyl3), and 2‐alkyl‐3‐amino4) substitution, have been evaluated for pharmacological activity.On the other hand, thiazolidone derivatives are reported to have anesthetic5), anticonvulsant6), and hypnotic7) activity.
Mechanismus der elektrochemischen Reduktion des Loprazolam (1) [6‐(2‐Chlorphenyl)‐2‐(4‐methyl‐1‐piperazinylmethylen)‐8‐nitro‐2H‐imidazol[1,2 a][1,4]benzodiazepin‐1H(4H)‐on] an einer Quecksilbertropfelektrode
Authors: Oelschläger Herbert , Volke Jiri , Vetter Michael Berthold , Schmidt Wolfgang 
Published: October 2006

AbstractLoprazolam (1) wird an der Quecksilbertropfelektrode in sauren Puffern (pH 2.8) in drei Stufen reduziert (DCT). Die erste Stufe (A) entspricht der Reduktion seiner NO2‐Gruppe zur Hydroxylaminostufe (4 Θ), die zweite Stufe (B) der Reduktion der °CN—‐Doppelbindung (5,6) (2 Θ), und die Stufe bei dem negativsten Potential (C) ist der Reduktion der Butazadiengruppierung zuzuordnen (4 Θ). Erst in stark sauren Puffern (pH < 2.8) wird auch die protonierte Hydroxylaminogruppe zu R‐NH2 reduziert, so daß sich unter dieser Bedingung ein Gesamtverbrauch von 12 Θ über alle Stufen ergibt.
Pyridazine Derivatives, VIII1): Synthesis and Antihypertensive Activity of 6‐(2‐Thienyl)‐5‐aminomethyl‐3‐hydrazino‐pyridazines
Authors: Ravina Enrique , Teran Carmen , Dominguez Neftali G. , Masaguer Christian F. , Gil‐Longo Jose , Orallo Francisco , Calleja Jose M. 
Published: October 2006

AbstractWe describe the synthesis by standard procedures of several 6‐(2‐thienyl)‐5‐aminomethyl‐3‐hydrazinopyridazines, and their α1‐blocking activity in isolated rat aorta and hypotensive effects in normotensive rats.
Synthesis of 6,7‐Dimethoxy Substituted 3,1‐Benzothiazin‐4‐ones
Authors: Gütschow Michael , Heinecke Kristina , Thiel Wilfried , Leistner Siegfried 
Published: October 2006

AbstractIn vorherigen Mitt.2,3) berichteten wir über die Synthese von 2‐Amino‐ bzw. Benzoylamino‐3,1‐benzothiazin‐4‐on (5 bzw. 4) sowie deren 6‐methyl‐ und 6‐Chlor‐Derivaten durch Einwirkung von konz. Schwefelsäure auf die ggf. 5‐substituierten 2‐(3‐Benzoylthioureido)benzoesäuren oder deren Methylester 1.
Pharmakokinetik von 5‐Fluorouracil nach i. v.‐Gabe unter Berücksichtigung der Erythrozyten
Authors: Czejka Martin , Schüller Johann , Fogl Ulrike 
Published: October 2006

AbstractDie in vivo Bindung des Zytostatikums 5‐Fluorouracil (1) an Erythrozyten wurde im Blut von Patienten untersucht. Der Einfluß der Erythrozyten auf die vaskuläre Verfügbarkeit von 1 beträgt (bezogen auf die AUC0–60‐Werte) 38. 6 ± 7. 2% für die Erythrozyten, der Erythrozytenverteilungskoeffizient beträgt 0. 65 ± 0. 18. Das Verteilungsvolumen und die totale Clearance von 1 werden durch die Erythrozyten erhöht, die Halbwertszeiten der Verteilung aus dem Kompartiment und der terminalen Elimination bleiben jedoch unberührt.
Synthesis and Preliminary Pharmacological Study of Thiophene Analogues of the Antipyretic and Analgesic Agent Ethenzamide
Authors: Darias V. , Bravo L. , Abdallah S. S. , Mateo C. C. Sánchez , Expósito‐orta M. A. , Lissavetsky J. , Manzanares J. 
Published: October 2006

AbstractA preliminary pharmacological study of a thiophene analogue 1b of the analgesic and antipyretic agent Ethenzamide and of a closely related compound 1a showed that a great similarity exists among Ethenzamide and the thiophenic compounds for analgesic, antipyretic, ulcerogenic, hypothermic, and sedative effects. However, the acute toxicity in mice for the thiophenic compounds is notably higher than that of Ethenzamide.
Dichloro‐[1‐(hydroxyphenyl)‐2‐phenylethylenediamine]platinum(II) Complexes: Testing on the Human Ovarian Cancer Cell Lines NIH: OVCAR 3 and SK OV 3
Authors: Bernhardt Günther , Müller Richard , Gust Ronald , Reile Herta , Keller Christoph , Spruß Thilo , Schönenberger Helmut 
Published: October 2006

AbstractThe diastereoisomeric dichloro‐[1‐(2‐, 3‐ and 4‐hydroxyphenyl)‐2‐phenyl‐ethylenediamine]platinum(II) complexes were tested on two human ovarian cancer cell lines NIH: OVCAR‐3 and SK‐OV‐3, both resistant against cisplatin. Dichloro‐[threo‐1‐(3‐hydroxyphenyl)‐2‐phenylethylenediamine]platinum(II) (threo‐5‐PtCl2) proved to be the most active representative of the new series, producing cytocidal effects at a concentration range of 2. 5 to 5. 0 μM on the NIH: OVCAR‐3 cell line. On the more resistant SK‐OV‐3 cell line, threo‐5‐PtCl2 was only moderately active, while in combination with BSO, a GSH level lowering compound, threo‐5‐PtCl2 showed a strong synergistic effect.