Synthesis, In Vitro Evaluations and Structure-Activity Assessment of Pyrrole Hydrazones as Potential Tuberculostatics

Publisher: Bentham Science Publishers

E-ISSN: 1875-628x|5|1|15-24

ISSN: 1570-1808

Source: Letters in Drug Design & Discovery, Vol.5, Iss.1, 2008-01, pp. : 15-24

Disclaimer: Any content in publications that violate the sovereignty, the constitution or regulations of the PRC is not accepted or approved by CNPIEC.

Previous Menu Next

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.