Title: Pyrrole-Based Hydrazones Synthesized and Evaluated In Vitro as Potential Tuberculostatics
Volume: 7
Issue: 6
Author(s): Atanas Bijev and Maya Georgieva
Affiliation:
Keywords:
Carbohydrazides, Hydrazones, Pyrrole, Synthesis, Tuberculostatics
Abstract: Twelve pyrrole hydrazones were synthesized and evaluated in vitro as inhibitors of Mycobacterium tuberculosis H37Rv with IC50 and IC90 to 5.92 μg/ml and 9.37 μg/ml respectively. The most active 12d (ethyl 5-(4-chlorophenyl)- 2-methyl-1-(4-(2-((5-nitrofuran-2-yl)methylene)hydrazinyl)-4-oxobutyl)-1H-pyrrole-3-carboxylate) has IC90 value of 9.372 μg/ml. The derived second order QSAR model favors moderate molecular surfaces in a combination with electronaccepting substituents in the aromatic hydrazone moiety.
