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Letters in Drug Design & Discovery

Editor-in-Chief

ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

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

Author(s): Atanas Bijev and Maya Georgieva

Volume 7, Issue 6, 2010

Page: [430 - 437] Pages: 8

DOI: 10.2174/157018010791306588

Price: $65

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


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