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Eur J Med Chem. 2014 Apr 22;77:231-42. doi: 10.1016/j.ejmech.2014.03.007. Epub 2014 Mar 5.

Acyl hydrazides and triazoles as novel inhibitors of mammalian cathepsin B and cathepsin H.

Author information

1
Department of Chemistry, Kurukshetra University, Kurukshetra, 136119, India. Electronic address: nraghav.chem@gmail.com.
2
Department of Chemistry, Kurukshetra University, Kurukshetra, 136119, India.

Abstract

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 (1)H NMR, (13)C 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 Ki values on purified cathepsin B and cathepsin H. The maximum inhibitory effect was exerted by 3-(3'-nitrophenyl)-5-(3'-nitrophenyl)-4-amino-1,2,4-triazoles (2c), 3-(4'-chlorophenyl)-5-(4'-chloro phenyl)-4-amino-1,2,4-triazoles (2h), 3-(3'-aminophenyl)-5-(3'-aminophenyl)-4-amino-1,2,4-triazoles (2i) and 4-methoxybenzohydrazide (1b).

KEYWORDS:

4-Amino-1,2,4-triazoles; Acyl hydrazides; Cathepsin B inhibitors; Cathepsin H inhibitors; Endogenous proteolysis

PMID:
24642566
DOI:
10.1016/j.ejmech.2014.03.007
[Indexed for MEDLINE]

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