Abstract
Fifteen new hydrazones were synthesized as derivatives of 1H-1-pyrrolylcarbohydrazides. Six products exhibited 73-98% inhibition against Mycobacterium tuberculosis H37Rv at 6.25 μg/mL using Microplate Alamar Blue Assay, the most active evaluated at HTS Level 2 with IC50=0.966 and IC90=3.236. The activities correlate with molecular volumes in simplified second order QSAR model.
Keywords: Carbohydrazides, Hydrazones, Pyrrole, QSAR, Synthesis, Tuberculostatics
Letters in Drug Design & Discovery
Title: Synthesis, In Vitro Evaluations and Structure-Activity Assessment of Pyrrole Hydrazones as Potential Tuberculostatics
Volume: 5 Issue: 1
Author(s): A. Bijev
Affiliation:
Keywords: Carbohydrazides, Hydrazones, Pyrrole, QSAR, Synthesis, Tuberculostatics
Abstract: Fifteen new hydrazones were synthesized as derivatives of 1H-1-pyrrolylcarbohydrazides. Six products exhibited 73-98% inhibition against Mycobacterium tuberculosis H37Rv at 6.25 μg/mL using Microplate Alamar Blue Assay, the most active evaluated at HTS Level 2 with IC50=0.966 and IC90=3.236. The activities correlate with molecular volumes in simplified second order QSAR model.
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Cite this article as:
Bijev A., Synthesis, In Vitro Evaluations and Structure-Activity Assessment of Pyrrole Hydrazones as Potential Tuberculostatics, Letters in Drug Design & Discovery 2008; 5 (1) . https://dx.doi.org/10.2174/157018008783406651
DOI https://dx.doi.org/10.2174/157018008783406651 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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