α-ketoheterocycles as inhibitors of Leishmania mexicana cysteine protease CPB was written by Steert, Koen;Berg, Maya;Mottram, Jeremy C.;Westrop, Gareth D.;Coombs, Graham H.;Cos, Paul;Maes, Louis;Joossens, Jurgen;Van der Veken, Pieter;Haemers, Achiel;Augustyns, Koen. And the article was included in ChemMedChem in 2010.Reference of 1826-13-7 This article mentions the following:
Cysteine proteases of the papain superfamily are present in nearly all eukaryotes and also play pivotal roles in the biol. of parasites. Inhibition of cysteine proteases is emerging as an important strategy to combat parasitic diseases such as sleeping sickness, Chagas disease, and leishmaniasis. Inspired by the in vivo antiparasitic activity of the vinylsulfone-based cysteine protease inhibitors, a series of α-ketoheterocycles were developed as reversible inhibitors of a recombinant L. mexicana cysteine protease, CPB2.8. Three isoxazoles and especially one oxadiazole compound are potent reversible inhibitors of CPB2.8; however, in vitro whole-organism screening against a panel of protozoan parasites did not fully correlate with the observed inhibition of the cysteine protease. In the experiment, the researchers used many compounds, for example, 5-Phenylthiazole (cas: 1826-13-7Reference of 1826-13-7).
5-Phenylthiazole (cas: 1826-13-7) belongs to thiazole derivatives. The thiazole ring is notable as a component of the vitamin thiamine (B1). The pyridine-type nitrogen in the thiazole ring deactivates the ring for electrophilic substitution reactions, which is further reduced in acid due to protonation of the thiazole ring.Reference of 1826-13-7
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica