Abstract
Twelve pyrrole hydrazones were synthesized and evaluated in vitro as inhibitors of Mycobacterium tuberculosis H37Rv with IC50 and IC90 to 5.92 μg/ml and 9.37 μg/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 μg/ml. The derived second order QSAR model favors moderate molecular surfaces in a combination with electronaccepting substituents in the aromatic hydrazone moiety.
Keywords: Carbohydrazides, Hydrazones, Pyrrole, Synthesis, Tuberculostatics
Letters in Drug Design & Discovery
Title: Pyrrole-Based Hydrazones Synthesized and Evaluated In Vitro as Potential Tuberculostatics
Volume: 7 Issue: 6
Author(s): Atanas Bijev and Maya Georgieva
Affiliation:
Keywords: Carbohydrazides, Hydrazones, Pyrrole, Synthesis, Tuberculostatics
Abstract: Twelve pyrrole hydrazones were synthesized and evaluated in vitro as inhibitors of Mycobacterium tuberculosis H37Rv with IC50 and IC90 to 5.92 μg/ml and 9.37 μg/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 μg/ml. The derived second order QSAR model favors moderate molecular surfaces in a combination with electronaccepting substituents in the aromatic hydrazone moiety.
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Cite this article as:
Bijev Atanas and Georgieva Maya, Pyrrole-Based Hydrazones Synthesized and Evaluated In Vitro as Potential Tuberculostatics, Letters in Drug Design & Discovery 2010; 7 (6) . https://dx.doi.org/10.2174/157018010791306588
DOI https://dx.doi.org/10.2174/157018010791306588 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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