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

Author: Bijev, A.

Source: Letters in Drug Design & Discovery, Volume 3, Number 7, September 2006 , pp. 506-512(7)

Publisher: Bentham Science Publishers

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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

Document Type: Research article

DOI: http://dx.doi.org/10.2174/157018006778194790

Affiliations: 1: University of Chemical Technology and Metallurgy, 8 “Kl. Ohridski” Blvd., 1756 Sofia, Bulgaria,USA.

Publication date: 2006-09-01

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