Synthesis, In Vitro Evaluations and Structure-Activity Assessment of Pyrrole Hydrazones as Potential Tuberculostatics
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.
Keywords: Carbohydrazides, Hydrazones, Pyrrole, QSAR, Synthesis, Tuberculostatics
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