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Syntheses,characterization,and evaluation of novel non-carboxylic analogues of Gemfibrozil:a bioisosteric approach

Syntheses, characterization, and evaluation of novel non-carboxylic analogues of Gemfibrozil:a bioisosteric approach

作     者:Nidhi Kala Anand Gaurav Vertika Gautam Nidhi Kala;Anand Gaurav;Vertika Gautam

作者机构:School of Pharmaceutical SciencesShobhit UniversityModipuramMeerut 250110lndia Faculty of Pharmaceutical SciencesUCSI UniversityNo.1UCSI HeightsJalan Menara GadingTaman ConnaughtKuala Lumpur 56000Federal Territory of Kuala Lumpur Department of ChemistryFaculty of ScienceUniversity of MalayaKuala Lumpur 50603Malaysia 

出 版 物:《Journal of Chinese Pharmaceutical Sciences》 (中国药学(英文版))

年 卷 期:2017年第26卷第2期

页      面:95-105页

核心收录:

学科分类:1007[医学-药学(可授医学、理学学位)] 100701[医学-药物化学] 10[医学] 

主  题:Atherosclerosis Coronary heart disease Fibrates Bioisosterism Hypolipidemic effect Gemfibrozil 

摘      要:Gemfibrozil is a widely used lipid modifying drug with well-established hypolipidemic and anti-atherosclerotic benefits; however, the presence of a carboxylic acid moiety in its structure is responsible for side effects in the gastrointestinal tract. The principle of bioisosterism was applied to design derivatives replacing the carboxylic acid group. The carboxylic acid group was replaced with bioisoteric groups, such as 1,2,4-triazole-3-thiol and hydroxamic acid. The derivatives were then synthesized, characterized, and evaluated in rats for reduced gastrointestinal irritation and hypolipidemic effects. Gemfibrozil was used as standard for comparison. The derivatives demonstrated less gastric irritation and retained hypolipidemic effects, however the hypolipidemic affects were significantly less than that of Gemfibrozil. The results of this study offers a direction for further research on the application of bioisosterism for the design of new derivatives of Gemfibrozil and other fibric acid derivatives.

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