Abstract:Derivatives of 1,3,4-oxadiazole are effective in the treatment and cure of a wide range of diseases in medical chemistry, while industrial development has shown that they can be utilised as corrosion inhibitors and light-emitting diodes. The researchers discovered several promising synthetic strategies that created 1,3,4-oxadiazoles in extraordinarily high yields while using environmentally friendly methods. These compounds can potentially be used in a wide range of lifechanging applications. Stable isomeric oxadiazole forms of pleconaril, raltegravir, butalamine, fasiplon, oxolamine, and several other drugs are among the numerous potent and effective pharmaceuticals that are now on the market. Fasiplon, butalamine, raltegravir, and pleconaril treat HIV/AIDS patients. This article has attempted to bring attention to the chemistry and pharmacology of oxadiazole and its derivatives. Oxadiazole derivatives have been used extensively as prospective therapeutic agents in clinical research, and this has become standard practice. The use of biological and in-silico models has enabled scientists to identify more synthetic analogues of cancer prevention, antifungal, and anti-HIV medications. This article provides recent information regarding procedures for synthesizing 1,3,4-oxadiazoles and their biological actions on the body.

01 Dec 2012·European review for medical and pharmacological sciencesQ4 · MEDICINE

Screening of differentially expressed genes and small molecule drugs of pediatric allergic asthma with DNA microarray.

Q4 · MEDICINE

Article

Author: Dong, L-Q ; Zhou, T-F ; Wang, X-M ; Wang, X-Q

BACKGROUNDAsthma is a disease resulting from a complex interaction of multiple genetic and environmental factors. More than 200 asthma candidate genes have been identified in the past decades by using genetic association studies, positional cloning and knockout mouse approaches.AIMThis study was to identify differentially expressed genes and provide direction for medicine design related to pediatric allergic asthma with DNA microarray.MATERIALS AND METHODSThe gene expression profile of pediatric allergic asthma GSE18965 was downloaded from Gene Expression Omnibus database which includes 16 samples, 7 normal and 9 pediatric allergic asthma samples. The differentially expressed genes between normal and disease samples were identified by using R language. The co-expression coefficient was calculated among the differentially expressed genes to construct co-expression networks with String Software. Software DAVID and FuncAssociate were used to analyze the functions of genes in the co-expression networks.RESULTSA total of 133 genes were identified as differentially expressed genes between normal and disease samples, and 8 related small medicine molecules were also obtained (penbutolol, felbinac, iodixanol, josamycin, oxolamine, 3-nitropropionic acid, scriptaid, and sanguinarine) from database CMAP. The differentially expressed genes were enriched in several biological processes, in which viral transcription and lysosome were the most significant GO term of up- or down-regulated genes.CONCLUSIONSOur present findings shed new light on the molecular mechanism of allergic asthma and provide three small molecular medicines (3-nitropropionic acid, scriptaid, and sanguinarine) which have the potential to use in clinic for treatment of allergic asthma in future.

01 Mar 2007·Biopharmaceutics & Drug DispositionQ4 · MEDICINE

Gender difference in the pharmacokinetic interaction between oral warfarin and oxolamine in rats: inhibition of CYP2B1 by oxolamine in male rats

Q4 · MEDICINE

Article

Author: Dae Y. Lee ; Wan G. Shin ; Xuan Zhu

AbstractThe possible reason for the significantly greater AUC of oral warfarin with oral oxolamine in male Sprague−Dawley rats was evaluated. After oral administration of warfarin at a dose of 2 mg/kg to male rats with oxolamine at doses of 10 and 50 mg/kg, the AUC values of warfarin were significantly greater than the controls (254 and 330 versus 180 µg h/ml). However, the AUC values of warfarin were not affected by oxolamine in female rats. This could be due to inhibition of CYP2B1, 2C11 and 3A2 by oxolamine in male rats, since warfarin was metabolized via CYP1A1, 2B1, 2C6, 2C11 and 3A2 in rats and CYP2B1 is male dominant, and CYP2C11 and 3A2 are male specific. Therefore, phenytoin, torasemide and clarithromycin (mainly metabolized via CYP2B1/2, 2C11 and 3A2 in rats, respectively) were administered intravenously to male rats with or without oral oxolamine. After oral oxolamine at doses of 10 and 50 mg/kg, the AUC of phenytoin was significantly greater (1280 and 1640 versus 938 µg min/ml), however, the AUC values of torasemide and clarithromycin were independent of oxolamine. The above data suggest that the significantly greater AUC of oral warfarin with oral oxolamine could be due to inhibition of CYP2B1/2 by oxolamine in male rats. Copyright © 2007 John Wiley & Sons, Ltd.

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