Lin, Cai published the artcileExploration of 6-methyl-7-(Hetero)Aryl-7-Deazapurine ribonucleosides as antileishmanial agents, Category: pyrazoles-derivatives, the publication is European Journal of Medicinal Chemistry (2022), 114367, database is CAplus and MEDLINE.
Leishmaniasis causes high mortality and morbidity in tropical and subtropical regions of Africa, Asia, the Americas and southern Europe, and is characterized by diverse clin. manifestations. The Leishmania parasite is deficient in de novo purine synthesis, and therefore acquires purines from the host and processes these using a purine salvage pathway. In vitro screening of an inhouse purine nucleoside library and analog synthesis afforded the 6-methyl-7-(2-pyridyl)-7-deazapurine ribonucleoside analog, e.g. I, as a promising hit. Encouraged by the favorable in vitro metabolic stability, an in vivo study was performed using an early curative L. infantum hamster model. When orally administrated at 50 mg/kg once daily (s.i.d) for 10 days, I was devoid of side effects, however, it only poorly reduced amastigote burdens in the major target organs.
European Journal of Medicinal Chemistry published new progress about 724710-02-5. 724710-02-5 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Boronic acid and ester,Pyrazole,Boronic Acids,Boronic acid and ester, name is (1H-Pyrazol-5-yl)boronic acid, and the molecular formula is C3H5BN2O2, Category: pyrazoles-derivatives.
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