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Letters in Drug Design & Discovery

Editor-in-Chief

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

New Heterocyclic Hydrazones in the Search for Antitubercular Agents: Synthesis and In Vitro Evaluations

Author(s): ">A. Bijev

Volume 3, Issue 7, 2006

Page: [506 - 512] Pages: 7

DOI: 10.2174/157018006778194790

Price: $65

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

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