64017-50-1Relevant academic research and scientific papers
Acyl hydrazides and triazoles as novel inhibitors of mammalian cathepsin B and cathepsin H
Raghav, Neera,Singh, Mamta
, p. 231 - 242 (2014/04/03)
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 1H NMR, 13C 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).
A facile and solvent-free synthesis of 3,5 -disubstituted-4-amino-1,2,4-triazoles by reactions of aromatic nitriles with hydrazine
Ikemi, Yukio,Hayashi, Naoto,Kakehi, Akikazu,Matsumoto, Kiyoshi
, p. 439 - 442 (2007/10/03)
A variety of 3, 5-disubstituted-4-amino-1,2,4-triazoles were prepared by reactions of aromatic nitriles with hydrazine monohydrate. The structure of 3,5-diphenyl-4-amino-1,2,4-triazole was established by an X-ray analysis.
Synthesis of 3,5-diaryl-4-benzylidene-amino-1,2,4-triazoles and 4-amino-3,5-diaryl-1,2,4-triazoles
Zielinski,Czardybon
, p. 1107 - 1110 (2007/10/03)
A one-pot reaction leading to 3,5-diaryl-4-benzylideneamino-1,2,4-triazoles is described, the key step of which is the reaction of arenecarbohydrazonoyl chloride with benzylidenehydrazide. Compounds obtained in this way were hydrolyzed to 4-amino-3,5-diaryl-1,2,4-triazoles.
A simple one step synthesis of new 3,5-disubstituted-4-amino-1,2,4- triazoles
Bentiss,Lagrenee,Traisnel,Mernari,Elattari
, p. 149 - 152 (2007/10/03)
A number of symmetrically 3,5-disubstituted 4-amino-1,2,4-triazoles have been prepared by the reaction of aromatic nitriles with hydrazine dihydrochloride or sulfate with an excess of hydrazine hydrate in ethylene or diethylene glycol under a nitrogen atm
