da Silva, Edson R. published the artcileNovel Selective Inhibitor of Leishmania (Leishmania) amazonensis Arginase, Category: triazoles, the main research area is Leishmania leishmaniasis leishmanicide; Leishmania; arginase; polyamines; triazolopyrimidine; trifluoromethyl; trypanothione.
Arginase is a glycosomal enzyme in Leishmania that is involved in polyamine and trypanothione biosynthesis. The central role of arginase in Leishmania amazonensis was demonstrated by the generation of two mutants: one with an arginase lacking the glycosomal addressing signal and one in which the arginase-coding gene was knocked out. Both of these mutants exhibited decreased infectivity. Thus, arginase seems to be a potential drug target for Leishmania treatment. In an attempt to search for arginase inhibitors, 29 derivatives of the [1,2,4]triazolo[1,5-a]pyrimidine system were tested against Leishmania amazonensis arginase in vitro. The [1,2,4]triazolo[1,5-a]pyrimidine scaffold containing CF3 substituent exhibited greater activity against the arginase compared to one with Me substituent in the 2-position. The novel compound I was the most potent, inhibiting arginase by a noncompetitive mechanism, with the Ki and IC50 values for arginase inhibition estimated to be 17±1 μM and 16.5±0.5 μM, resp. These results can guide the development of new drugs against leishmaniasis based on [1,2,4]triazolo[1,5-a]pyrimidine derivatives targeting the arginase enzyme.
Chemical Biology & Drug Design published new progress about Homo sapiens. 24415-66-5 belongs to class triazoles, name is 7-Chloro-5-methyl-[1,2,4]triazolo[1,5-a]pyrimidine, and the molecular formula is C6H5ClN4, Category: triazoles.
Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics