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
Letters in Drug Design & Discovery
Title: New Pyrrole Hydrazones Synthesized and Evaluated In Vitro as Potential Tuberculostatics
Volume: 6 Issue: 7
Author(s): A. Bijev, S. Vladimirova and P. Prodanova
Affiliation:
Keywords: Carbohydrazides, Hydrazones, Pyrrole, Synthesis, Tuberculostatics
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.
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Cite this article as:
Bijev A., Vladimirova S. and Prodanova P., New Pyrrole Hydrazones Synthesized and Evaluated In Vitro as Potential Tuberculostatics, Letters in Drug Design & Discovery 2009; 6 (7) . https://dx.doi.org/10.2174/157018009789108268
DOI https://dx.doi.org/10.2174/157018009789108268 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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