Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 77, Issue -, Pages 231-242Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2014.03.007
Keywords
Acyl hydrazides; 4-Amino-1,2,4-triazoles; Cathepsin B inhibitors; Cathepsin H inhibitors; Endogenous proteolysis
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Funding
- CSIR New Delhi, India
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In the past decade, the work on the identification of small molecular weight compounds as inhibitors of cysteine proteases has been in focus. In this direction, we here present the facile microwave assisted synthesis of some acyl hydrazides and triazoles, followed by their evaluation as protease inhibitors and inhibitory studies on cathepsin B and cathepsin H, two significant lysosomal cysteine proteases. The compounds were characterized by H-1 NMR, C-13 NMR, Mass and IR spectral data. The compounds which were found inhibitory to endogenous proteolysis in liver homogenate at pH 5.0 were further studied for determination of inhibition type and IC; values on purified cathepsin B and cathepsin H. The maximum inhibitory effect was exerted by 3-(3'-nitropheny1)-5-(3'-nitrophenyI)-4-amino-1,2,4-triazoles (2c), 3(4'-chlorophenyI)-5-(4'-chloro phenyl)-4-amino-1,2,4-triazoles (2h), 3-(3'-aminopheny1)-5-(3'-aminopheny1)-4-amino-1,2,4-triazoles (2i) and 4-methoxybenzohydrazide (lb). (c) 2014 Elsevier Masson SAS. All rights reserved.
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