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Letters in Drug Design & Discovery

Author(s): A. Bijev, S. Vladimirova and P. Prodanova

DOI: 10.2174/157018009789108268

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New Pyrrole Hydrazones Synthesized and Evaluated In Vitro as Potential Tuberculostatics

Page: [508 - 517] Pages: 10

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Abstract

Sixteen hydrazones were synthesized as derivatives of 1H-1-pyrrolylcarbohydrazides. Five products exhibited 68-97% inhibition against Mycobacterium tuberculosis H37Rv at 6.25 μg/mL using MABA, the most active displaying IC50=7.979 μg/mL and IC90 > 100 μg/mL. Activities correlated with the hydrophobic parameters according to second order QSAR model favoring 4.4 LogP 5.2.

Keywords: Carbohydrazides, Hydrazones, Pyrrole, Synthesis, Tuberculostatics