Abstract
Sixteen pyrrole containing hydrazones were synthesized from isoniazid (INH) or from 1H-1- pyrrolylcarbohydrazides. Nine products exhibited 92-100% inhibitory activity against Mycobacterium tuberculosis H37Rv at 6.25 μg/mL (Microplate Alamar Blue Assay). Two leads showed MICs 0.78 and > 0.1 μg/mL, SIs > 12.82 and > 100. "Drug likeness" was assessed by "Lipinski rule of five".
Keywords: Carbohydrazides, Hydrazones, Pyrrole, Synthesis, Tuberculostatics
Letters in Drug Design & Discovery
Title: New Heterocyclic Hydrazones in the Search for Antitubercular Agents: Synthesis and In Vitro Evaluations
Volume: 3 Issue: 7
Author(s): A. Bijev
Affiliation:
Keywords: Carbohydrazides, Hydrazones, Pyrrole, Synthesis, Tuberculostatics
Abstract: Sixteen pyrrole containing hydrazones were synthesized from isoniazid (INH) or from 1H-1- pyrrolylcarbohydrazides. Nine products exhibited 92-100% inhibitory activity against Mycobacterium tuberculosis H37Rv at 6.25 μg/mL (Microplate Alamar Blue Assay). Two leads showed MICs 0.78 and > 0.1 μg/mL, SIs > 12.82 and > 100. "Drug likeness" was assessed by "Lipinski rule of five".
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Bijev A., New Heterocyclic Hydrazones in the Search for Antitubercular Agents: Synthesis and In Vitro Evaluations, Letters in Drug Design & Discovery 2006; 3 (7) . https://dx.doi.org/10.2174/157018006778194790
DOI https://dx.doi.org/10.2174/157018006778194790 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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