bluuebunny/crossref_metadata_2025_split huggingface dataset:
A Gold‐Catalyzed A3 Coupling/Cyclization/Elimination Sequence as Versatile Tool for the Synthesis of Furfuryl Alcohol Derivatives from Glyceraldehyde and Alkynes
Authors: Li Jian , Rudolph Matthias , Rominger Frank , Xie Jin , Hashmi. A. Stephen K. 
Published: January 2016

AbstractThe reaction of glyceraldehyde with alkynes delivers furfuryl alcohol derivatives within only one reaction step in the presence of a gold(III) catalyst. The reaction cascade is initiated by an intermolecular gold‐catalyzed A3 coupling sequence in which morpholine is used as additive. Intramolecular cyclization and subsequent aromatization under elimination of the amine then deliver the target molecules. The protocol offers a valuable alternative to the common routes that are based on functionalization of already existing furan cores.magnified image
Hollow‐Structured Carbon‐Supported Nickel Cobaltite Nanoparticles as an Efficient Bifunctional Electrocatalyst for the Oxygen Reduction and Evolution Reactions
Authors: Wang Jie , Wu Zexing , Han Lili , Lin Ruoqian , Xin Huolin L. , Wang Deli 
Published: January 2016

AbstractThe exploration of efficient electrocatalysts for both the oxygen reduction reaction (ORR) and oxygen evolution reaction (OER) is essential for fuel cells and metal‐air batteries. In this study, we developed 3 D hollow‐structured NiCo2O4/C nanoparticles with interconnected pores as bifunctional electrocatalysts, which are transformed from solid NiCo2 alloy nanoparticles through the Kirkendall effect. The unique hollow structure of NiCo2O4 nanoparticles increases the number of active sites and improves contact with the electrolyte to result in excellent ORR and OER performances. In addition, the hollow‐structured NiCo2O4/C nanoparticles exhibit superior long‐term stability for both the ORR and OER compared to commercial Pt/C. The template‐ and surfactant‐free synthetic strategy could be used for the low‐cost and large‐scale synthesis of hollow‐structured materials, which would facilitate the screening of high‐efficiency catalysts for energy conversion.
Selective β‐Arylation of Thiophenes with Aryl Iodides Catalyzed by Dinuclear Palladium Carboxylate Complexes
Authors: Maki Yohei , Goto Takahiro , Tsukada Naofumi 
Published: January 2016

AbstractNovel dinuclear palladium complexes bearing acetoxy ligands were synthesized and characterized by X‐ray crystal analysis. The complexes were utilized for the arylation of 2‐ethylthiophene with iodobenzene to give ethylphenylthiophenes with high β selectivity. The β‐arylation was also applied to a variety of iodoarenes and thiophenes, except those bearing conjugated carbonyl substituents.
Copper–Manganese Spinel Oxide Catalyzed Synthesis of Amides and Azobenzenes via Aminyl Radical Cations
Authors: Sultan Shaista , Kumar Manjeet , Devari Shekaraiah , Mukherjee Debaraj , Ali Shah Bhahwal 
Published: January 2016

AbstractA highly efficient Cu–Mn‐catalyzed process for the aminolysis of esters was developed. Also, the catalyst promoted the self‐ and cross‐dehydrogenative coupling of anilines to generate symmetrical and unsymmetrical azobenzenes, respectively. The reactions were performed under neutral conditions with an inexpensive catalyst, gave high yields, and offered wide functional group tolerance.
Doubly Cavitand‐Capped Porphyrin Capsule by Hydrogen Bonds
Authors: Kishimoto Kazuki , Nakamura Munechika , Kobayashi Kenji 
Published: January 2016

AbstractThe components of a 1:2 mixture of meso‐tetrakis(4‐dodecyl‐3,5‐dihydroxyphenyl)porphyrin (1) and a bowl‐shaped tetrakis(4‐pyridylethynyl)cavitand (2) in CDCl3 or C6D6 self‐assemble quantitatively into the doubly cavitand‐capped porphyrin capsule 2⋅1⋅2 through eight ArOH⋅⋅⋅Npy hydrogen bonds. Capsule 2⋅1⋅2 possesses two cavities divided by the porphyrin ring and encapsulates two molecules of 1‐acetoxy‐3,5‐dimethoxybenzene (G) as a guest to form G/G@(2⋅1⋅2). Remarkable solvent effect was observed, in which the apparent association constant of 2⋅1⋅2 with G in C6D6 was much greater than that in CDCl3.
Welche Wünsche und Erwartungen haben Lehrkräfte an aktuelle Forschung als Gegenstand von Fortbildungsveranstaltungen?
Authors: Ropohl Mathias , Schönau Katharina , Parchmann Ilka 
Published: January 2016

AbstractZiel des Fortbildungsprogramms „Transfer Wissenschaft → Schule“ ist die Vorstellung aktueller Forschungsfelder und ‐methoden der Wissenschaft mit Bezügen zu naturwissenschaftlichen Fächern in Fortbildungsveranstaltungen für Lehrkräfte. Im Vorfeld der Konzeption verschiedener Angebote wurden Lehrkräfte in Schleswig‐Holstein nach ihren Erfahrungen und Entwicklung bezüglich dieses Fortbildungsinhaltes befragt. In diesem Beitrag werden die Ergebnisse der erhobenen Daten von N=273 Lehrkräften für naturwissenschaftliche Fächer aus Schleswig‐Holstein mit Blick auf Unterrichtsthemen bzw. ‐kontexte sowie Aspekte der Forschungsprozesse berichtet. Dabei zeigt sich unter anderem, dass sich Lehrkräfte beispielsweise aktuelle Forschungsfragen als Gegenstand von Angeboten wünschen, die Thematisierung der Person der Forscherin bzw. des Forschers jedoch deutlich geringer gewichtet wird. Abschließend werden in dem Beitrag Konsequenzen aus der Befragung für das Fortbildungsprogramms „Transfer Wissenschaft → Schule“ erläutert, welches derzeit in Schleswig‐Holstein realisiert wird.
Localized Plasmon‐Stimulated Nanochemistry of Graphene Oxide on a SERS Substrate
Authors: Ramanauskaite Lina , Xu Huizhong , Snitka Valentinas 
Published: January 2016

AbstractIn recent years, there has been remarkable progress in the reduction and functionalization of graphene oxide (GO) using nanoparticles and high‐energy optical photons. Most of these reactions are carried out in solutions, whereas the local modification of GO on solid substrates still remains a challenge. In this work, we demonstrate the local reduction of GO and its further destruction, leading to the synthesis of polyaromatic hydrocarbons (PAHs) stimulated by localized surface plasmons (LSPs). The reduction of GO and the synthesis of PAHs have been carried out on a substrate designed for surface‐enhanced Raman spectroscopy (SERS). We found that LSPs initiate the destruction of water molecules entrapped in the nanogaps between silver nanoparticles after the deposition of GO from the aqueous suspension. It was demonstrated that OH radicals, as a result of water decomposition, initiate the reduction of GO, leading to the synthesis of PAHs. The reactions have been observed in real time by using SERS. The measurement of current–voltage (I–V) characteristics through conductive atomic force microscopy (AFM), recorded in an LSP‐stimulated area, have shown the increased electrical conductivity (more than ten times) compared with the conductivity of GO. The synthesis of new compounds in the LSP‐stimulated area has been confirmed by the appearance of new peaks in the Raman spectra and nonlinear I–V characteristics typical for PAHs. We show that the used method allows the local modification of electrical properties of GO and controlled nanopattering of organic compounds on the surface.
Developing and testing of new drugs by the pharmaceutical industry
Authors: Kohlstaedt Kenneth G. 
Published: January 2016

The developing and testing of new drugs is an important responsibility of the pharmaceutical industry. The first tests are “screening” procedures that are intended to Uncover leads indicating possible therapeutic usefulness. After thorough pharmacologic and toxicity testing in experimental animals, a new drug is ready for the initial trial in a human subject.It is practical for a pharmaceutical manufacturer to maintain a clinical research unit and a staff of investigators for performance of the initial human trials. A new therapeutic agent is then placed in the hands of a limited number of experienced and qualified investigators so that adequately controlled studies can be conducted under dose observation. In some instances, as a final evaluation, the drug is subjected to a broad clinical trial by a Zarge number of physicians. If properly conducted, important information can be obtained by the use of a drug tmder conditions found in the practice of medicine. Evidence of hypersensitivity cannot be detected by limited trial. The dinical investigator must plan the study wilh great attention to detail. Every effort must be made to avoid bias.In the development of the drug the tcork of the pharrnaceutical chemist is important in preparing a satisfactory dosage form; the control division must establish criteria for the composition of the ingredients as well as for the final product and must prove the stability. Publication of reports in the scientific journals must include methods and controls for clinical studies and the results. A group of investigators can use one experimental design and pool the findings in a single paper. The investigator should report all data to the manufactllrer as quickly as possible.
Metabolic effects and therapeutic applications of triiodothyropropionic acid
Authors: Leeper Robert D. , Mead Allen W. , Money William L. , Rawson Rulon W. 
Published: January 2016

The effects of mare than sixty analogues of thyroxine have been investigated in animals, and more than thirty analogues have been studied in humans. Animal studies have shown that structural alterations of the thyroid hormone cause not only large variations in potency but also dissociation of the various hormonal effects of thyroxine. Dissociation of thyroid horrrwnal effects has also been demonstrated in the human with triiodothyropropionic acid.The drug is satisfactory as maintenance therapy in myxedema and appears to have definite advantages in maintaining the myxedematous patient with angina pectoris. Triiodothyropropionic acid effects a 15 to 20 per cent drop in the serum cholesterol of about 80 per cent of euthyroid individuals with either elevated or normal cholesterol levels. Its administration in the proper dosage decreases elevated serum uric acid levels in both myxedematous and euthyroid individuals.
A clinical evaluation
Authors: Vosti Gordon J. , Willett Forrest M. , Jawetz Ernest 
Published: January 2016

Demethylchlortetracycline, a recently available member of the tetracycline group of antibiotics, has been evaluated clinically in 59 patients seen in a Veterans Administration Hospital with infections of the lower respiratory tract, urinary tract, or skin. The drug appeared to be comparable to other tetracyclines, and if the isolated etiologic organism was sensitive to DMCT in vitro, patients generally responded favorably. The study illustrated the great difficulty facing the physician who attempts to evaluate a new antimicrobial drug which closely resembles other good drugs. A ma;ority of patients with infection suffered from underlying illnesses which predisposed them to infection or modified the infectious process through alteration of anatomic or physiologic host conditions. In this complex situation, the suppression of microbial growth‐the sole effect of an antibiotic‐contributes only to a variable and unpredictable extent to the relief of symptoms and signs of infection.Among undesirable effects of oral DMCT administration were prominent gastrointestinal upsets with doses in excess of 600 mg. daily and a suggestion of renal and hepatic function impairment, which requires further study.
Some effects of nicotine and smoking on metabolic functions
Authors: larson P. S. , Haag H. B. , Silvette H. 
Published: January 2016

A number of the metabolic effects of nicotine (or tobacco smoke) reported in mammals are reviewed, and attention is drawn to the relative deficiency in this area of investigation. The suggestion is made that, concomitant with the advance of newer and more sophisticated biochemical and biophysical techniques, the effects of nicotine be more systematically studied using concentrations that include those encountered in man.In general, nicotine appears capable of increasing heat production, oxygen consumption, metabolic rate, and blood sugar. Studies of tissue metabolism show that nicotine can inhibit pyruvate oxidation by inhibiting specifically pyruvic dehydrogenase. Nicotine has been shown to possess anticholinesterase activity and to suppress acetylcholine synthesis. These observations may all be of importance in finally elucidating the mechanism of the neurotropic action of nicotine and deserve to be extended.The uncomplicated effect of nicotine on serum cholesterol and lipoprotein levels is not yet clearly apparent. Generally, the levels appear to be higher in smokers than in nonsmokers; the reason for the difference is obscure. Effects of nicotine on nitrogen metabolism are virtually unknown; effects on mineral metabolism, when demonstrable, appear indirect and to lack both consistency and significance. Vitamin metabolism is largely unaffected, except for ascorbic acid, which reportedly may be depleted to a perhaps significant extent.It is interesting and significant to note that there are few clinical reports which implicate nicotine (or tobacco smoke) etiologically or otherwise in deficiency or metabolic disorders.
Some effects of a new antiarrhythmie drug
Authors: Kahn Hyman R. , Lewis Daniel W. , Killough John H. , Abrams William B. 
Published: January 2016

The effects of RO 2‐5803, a compound shown to have antiarrhythmic properties in animals, were studied in 13 patients with atrial flutter or fibrillation. After a single oral dose, the atrial rate was slowed as much as 39 per cent; the efJect lasted up to 24 hours. Intravenous administration produced similar effects with smaller doses.After large oral doses, mild gastrointestinal disturbances were sometimes noted. Intravenous administration usually was followed by a transient, mild drop in blood pressure. One episode of severe hypotension occurred. There were no other untoward effects.RO 2‐5803 and quinidine caused similar slowing of the atrial rate. The drugs differed mainly in their effect on the ventricular rate. The cause of the ventricular slowing after RO 2‐5803 administration is not clear. Further study is required to determine whether it is secondary to the slower atrial rate, because of direct depression of the A‐V node or of a vagallike action.
Nerve iniury from intramuscular barbiturate iniection
Authors: Richards Richard K. 
Published: January 2016

Intramuscular injection of drugs is usually considered a safe procedure. Occasionally, however, nerve damage, particularly to the sciatic nerve, has been reported following various drugs. There has been same dispute regarding the role which the chemical nature of the drug, the simple physical pressure effect, and technique play in such incidents.A case is reported in which definite sensory damage to the sciatic nerve occurred in a patient after the intragluteal administration of amobarbital sodium. Experiments were undertaken in which amobarbital sodium solution was iniected along the course of the sciatic nerve in guinea pigs. Hypalgesia and decrease of muscle tone developed in all instances, and in same of the animals trophic changes of the feet appeared. The need for careful technique in placing the intramuscular iniection outside the course of the sciatic nerve is discussed.
Factors affecting the absorption and biliary excretion of erythromycin and two of its derivatives in humans
Authors: Hammond James B. , Griffith R. S. 
Published: January 2016

The oral administration of the propionyl ester of erythromycin and the lauryl sulfate salt of the ester produces higher serum concentrations than the parent antibiotic, erythromycin. Lee explained this by his findings in rats that the biliary excretion of erythromycin was relatively high while that of the two derivatives was low. We extended his work to humans.In 16 patients, with bile fistula propionyl erythromycin administered orally was followed by relatively high serum and low bile antibiotic activity, as compared to erythromycin. The lauryl sulfate salt form followed a pattern similar to the ester. Diverting antibiotic‐containing bile from the intestine lowered the serum antibiotic concentration during treatment with erythromycin. However, this procedure had little effect on the two derivatives, since they appear in the bile in only a minimal amount.The clinical findings support the animal data.
Clinical pharmacology of hypnotics and sedatives
Authors: Shideman F. E. 
Published: January 2016

If there is any tendency to become complacent about the adequacy of knowledge in a given area, a review of the subject usually serves to dispel this attitude. Although there exists a formidable body of knowledge on the pharmacology of the hypnotics and sedatives, that which remains unknown is even more formidable. Many of the experiments which have yielded information on the pharmacodynamics and disposition of these drugs in laboratory animals do not have their counterparts in human studies. In such instances, only a logical guess can be made in an effort to bridge this gap. The known effects of the barbiturates, bromides, paraldehyde, chloral hydrate, and newer hypnotics and sedatives in man are presented and an attempt is made to compare these with findings in other species. Where data of a critical nature with respect to the human pharmacology of these drugs are lacking, the fundamental features of their actions on other animals are presented.In addition to the more classic aspects of their pharmacodynamics, the more significant alterations in behavior produced by these agents are summarized. Studies dealing with their pharmacology in both the normal and pathologic states and in therapeutic and toxic dosages are outlined. Finally, the disposition of these compounds in the body is considered, inasmuch as this aspect of their pharmacology may have important bearing on the responses elicited by them in the organism.
III. The interaction of thiopental and oxymorphone during surgical anesthesia
Authors: Keeri-Szanto M. , Knaff M. , Rondeau Y. 
Published: January 2016

An equipotent mixture of thiopental and oxymorphone was used with very satisfactory results to supplement nitrous oxide anesthesia in 44 cases of major surgical operation. The mixture proved easy to prepare and to handle.The mean anesthetic time/dose curve was established for this mixture and compared with corresponding data obtained earlier for the component drugs. According to the mathematical analysis, the anesthetic action of the thiopental‐oxymorphone mixture is additive rather than synergistic.A technique is presented for the semiquantitative rating of various anesthetic agents, and by these criteria, the thiopental‐oxymorphone mixture is a better intravenous anesthetic agent than either of the components.
Behavioral patterns of anti barbituric action after 5‐phenyl‐2‐imino‐4‐oxo‐oxazolidine, amphetamine, and caffeine
Authors: Dureman Ingmar 
Published: January 2016

A battery of objective behavioral tests was used to assay the differential patterning of antibarbituric effects of 5‐phenyl‐2‐imino‐4‐oxo‐oxazolidine (PIO), amphetamine, and caffeine. The test battery included a difficult code‐tracking operation performed under forced speed conditions, a 40 minute monotonous test of clerical speed (simple arithmetic operations), reaction time, two tests of fine motor coordination, aiming accuracy (moving targets rotated at three different speed levels), and the Archimedes spiral. Pulse rate and systolic blood pressure were recorded before and after each session on the code‐tracking test.Two types of barbiturates (amobarbital and neopentylallylbarbituric acid) administered at two different dose levels (200 and 400 mg.) were given orally as hypnosedative premedication 150 minutes before the intake of the stimulant drugs. When compared with barbiturate plus placebo, PIO was found to differ from amphetamine and, to a slightly lesser degree, from caffeine in (1) having no antagonistic influence on residual pulse and blood pressure effects induced by barbiturate premedication, (2) having a less‐pronounced effect on variables related to visual motion aftereffect and finger‐hand dexterity, (3) being more effective in preserving a high level of operational skill against speed stress both in rotor aiming and a difficult learning variant of the code‐tracking test, and (4) being free of adverse effects from the subjective point of view.
Suppressive therapy of chronic bronchial infections
Authors: Dowling Harry F. , Lepper Mark H. , Jackson George Gee 
Published: January 2016

The studies of long‐term antibiotic therapy reported in the literature are reviewed. The best clinical and bacteriologic results were obtained with 1 to 2 Gm. of tetracycline administered each day. Lesser degrees of improvement were reported when smaller doses were given, when the antibiotic was administered twice a week, or when therapy was given for a portion of the year only. Penicillin therapy was considerably less effective, erythromycin therapy appeared totally ineffective, and oleandomycin‐penicillin therapy was more effective than penicillin but less so than tetracycline.Untoward reactions occurred in all regimens but, prOvided patients reported them promptly, were not serious. Tetracycline‐resistant staphylococci appeared in the sputum of an occasional patient during therapy with that antibiotic but did not cause any complications, except possibly the development of pneumonia in 1 patient.
Pathologic physiology, pharmacology, and therapeutics of tetanus
Authors: Laurence D. R. , Webster, R. A. 
Published: January 2016

Experimental evidence for the routes of tramport of tetanus toxin from the site of its formation to the central nervous system is reviewed. The possible sites and mechanisms of action of toxin are discussed, and an attempt is made to correlate the mode of action with that of drugs used to suppress convulsions.Despite the total absence until recently of any valid therapeutic comparisom, an attempt is made to evaluate the principal controversial therapeutic techniques, including antitoxin, care of the wound, chemotherapy, central anticonvulsants, neuromuscular blocking agents, tracheostomy, and adrenocortical steroids.
Part III. Chemistry, host entry, and metabolic fate of carcinogens
Authors: Falk Hans L. , Kotin Paul 
Published: January 2016

The skin, respiratory tract, and gastrointestinal tract are the organ systems through which environmental carcinogenic agents gain entry into the host. Of the several sources of carcinogenic agents, this report is concerned with the two most common in the respiratory environment—urban polluted air and cigarette smoke. Carcinogenic polycyclic aromatic hydrocarbons (PAH) are the most ubiquitous and are present in the highest concentrations. Certain exogenous and endogenous factors significantly modify the biologic action of carcinogenic hydrocarbons. Exogenous factors includes (1) the simultaneous presence and action of anticarcinogenic agents in the environment, (2) their occurrence in a physical state compatible with inhalation and deposition in the respiratory tract, and (3) the presence of factors modifying the host response, particularly in relation to the normal physiologic defenses. The endogenous factors include: (1) the vehicle serving the carcinogenic agents as it affects persistence at site of entry and rate of systemic distribution, (2) the rate of metabolism in the hepatobiliary system, and (3) the existence of anatomic or metabolic abnormalities modifying the tissue response.The metabolism of carcinogenic P AH is, in the truest sense, a pharmacologic detoxification process since the metabolites are either weakly or, as is more common, wholly noncarcinogenic. This suggests that carcinogenic PAH, as they occur in the environment, are the proximate carcinogens. The complexity of the carcinogenic process is emphasized by the multiplicity of factors, many of them noncarcinogenic in themselves, that are concerned with the pathogenesis of neoplastic disease.