52868-19-6Relevant 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).
Synthesis and biological evaluation of some novel 3,5-disubstituted-1,2,4- triazole incorporated 2-mercaptobenzothiazoles
Azam, Mohammed Afzal,Suresh, Bhojraj,Srinivas, Naga,Sachdev, Sumit,Rajeshkumar, Raman
, p. 739 - 748 (2013/02/22)
Several 2-mercaptobenzothiazole derivatives 5a-i containing 1,2,4-triazole moiety incorporating two additional substituents were synthesized. All the newly synthesized compounds were tested for in vitro activity against certain strains of bacteria such as Enterococcus faecalis, Bacillus coagulans, Pseudomonas aeruginosa, Escherichia coli and Candida albicans. Compound 5a showed significant activity against the Gram-negative bacteria Escherichia coli. Compounds 5a-i were also screened for their antifungal activity against Candida albicans and compounds 5a, 5b, 5d and 5g displayed significant activity against this fungus. Some of these compounds were evaluated for their in vivo anti-inflammatory activity, acute toxicity and ulcerogenic actions. Tested compounds 5g and 5h showed significant anti-inflammatory activity and significant gastrointestinal protection compared to the standard drug diclofenac sodium. Molecular modeling studies of the synthesized compounds are presented.
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.
High-throughput synthesis of symmetrically 3,5-disubstituted 4-amino-1,2,4-triazoles from aldehydes using microwave
Koshima, Hideko,Hamada, Mitsuo,Tani, Makiko,Iwasaki, Shunsuke,Sato, Fumika
, p. 2145 - 2148 (2007/10/03)
Symmetrically 3,5-substituted 4-amino-1,2,4-triazoles are quickly prepared from aromatic aldehydes via nitriles by two-step reactions without any separation under microwave irradiation for each several minutes.
Accelerated synthesis of 3,5-disubstituted 4-amino-1,2,4-triazoles under microwave irradiation
Bentiss, Fouad,Lagrenée, Michel,Barbry, Didier
, p. 1539 - 1541 (2007/10/03)
A number of symmetrically 3,5-disubstituted 4-amino-1,2,4-triazoles are quickly prepared by the reaction of aromatic nitriles on hydrazine dihydrochloride in the presence of an excess of hydrazine hydrate in ethylene glycol under microwave irradiation. (C
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
