Pyrrole-Based Hydrazones Synthesized and Evaluated In Vitro as Potential Tuberculostatics

被引：17

作者：

Bijev, Atanas ^{[1
]}

Georgieva, Maya ^{[1
]}

机构：

[1] Univ Chem Technol & Met, Dept Organ Synth & Fuels, BU-1756 Sofia, Bulgaria

来源：

LETTERS IN DRUG DESIGN & DISCOVERY | 2010年 / 7卷 / 06期

关键词：

Carbohydrazides; Hydrazones; Pyrrole; Synthesis; Tuberculostatics; MYCOBACTERIUM-TUBERCULOSIS; DERIVATIVES; AGENTS;

D O I：

10.2174/157018010791306588

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Twelve pyrrole hydrazones were synthesized and evaluated in vitro as inhibitors of Mycobacterium tuberculosis H(37)Rv with IC50 and IC90 to 5.92 mu g/ml and 9.37 mu g/ml respectively. The most active 12d (ethyl 5-(4-chlorophenyl)-2-methyl-1-(4-(2-((5-nitrofuran-2-yl)methylene)hydrazinyl)-4-oxobutyl)-1H-pyrrole-3-carboxylate) has IC90 value of 9.372 mu g/ml. The derived second order QSAR model favors moderate molecular surfaces in a combination with electron-accepting substituents in the aromatic hydrazone moiety.

引用

页码：430 / 437

页数：8

共 14 条

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