Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
USA
Email: lddd@benthamscience.org

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

Author(s): A. Bijev.

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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Article Details

VOLUME: 3
ISSUE: 7
Year: 2006
Page: [506 - 512]
Pages: 7
DOI: 10.2174/157018006778194790
Price: $58