Novel acyl coenzyme A: diacylglycerol acyltransferase 1 inhibitors-synthesis and biological activities of N-(substituted heteroaryl)-4-(substituted phenyl)-4-oxobutanamides was written by Nakada, Yoshihisa;Ogino, Masaki;Asano, Kouhei;Aoki, Kazuko;Miki, Hiroshi;Yamamoto, Toshihiro;Kato, Koki;Masago, Minori;Tamura, Norikazu;Shimada, Mitsuyuki. And the article was included in Chemical & Pharmaceutical Bulletin in 2010.Category: thiazole This article mentions the following:
In a program to discover new small mol. diacylglycerol acyltransferase (DGAT)-1 inhibitors, screening of our inhouse chem. library was carried out using recombinant human DGAT-1 enzyme. From this library, the lead compound 1a (I) was identified as a new class of DGAT-1 inhibitor. A series of novel N-(substituted heteroaryl)-4-(substituted phenyl)-4-oxobutanamides 2 was designed from 1a, synthesized and evaluated for inhibitory activity against DGAT-1 enzyme. Among these compounds, N-(5-benzyl-4-phenyl-1,3-thiazol-2-yl)-4-(4,5-diethoxy-2-methylphenyl)-4-oxobutanamide 9 was found to exhibit potent inhibitory activity and good enzyme selectivities. Following administration in KKAy mice with 3 mg/kg high fat diet admixture for four weeks, 9 reduced body weight gain and white adipose tissue weight without affecting total food intake. These results suggested that the small mol. DGAT-1 inhibitor might have potential in the treatment of obesity and metabolic syndrome. In the experiment, the researchers used many compounds, for example, 4,5-Diphenylthiazol-2-amine (cas: 6318-74-7Category: thiazole).
4,5-Diphenylthiazol-2-amine (cas: 6318-74-7) belongs to thiazole derivatives. Thiazole is a five-membered, unsaturated, planar, π-excessive heteroaromatic containing one sulfur atom and one pyridine-type nitrogen atom at position 3 of the cyclic ring system. Electrophilic attack at nitrogen depends on the presence of electron density at nitrogen as well as the position and nature of substituent linked to the thiazole ring.Category: thiazole
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica