Synthesis and biological evaluation of thiazole derivatives as GPR119 agonists was written by Kim, Hyojin;Cho, Suk Joon;Yoo, Minjin;Kang, Seung Kyu;Kim, Kwang Rok;Lee, Hwan Hee;Song, Jin Sook;Rhee, Sang Dal;Jung, Won Hoon;Ahn, Jin Hee;Jung, Jae-Kyung;Jung, Kwan-Young. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2017.Electric Literature of C11H20N2O2S This article mentions the following:
A series of 4-(phenoxymethyl)thiazole derivatives was synthesized and evaluated for their GPR119 agonistic effect. Several 4-(phenoxymethyl)thiazoles with pyrrolidine-2,5-dione moieties showed potent GPR119 agonistic activities. Among them, compound I (R = F, Me) showed good in vitro activity with an EC50 value of 49 nM and 18 nM, resp. with improved human and rat liver microsomal stability compare with MBX-2982. Compound I (R = F, Me) did not exhibit significant CYP inhibition, hERG binding, and cytotoxicity. Moreover, these compounds lowered the glucose excursion in mice in an oral glucose-tolerance test. In the experiment, the researchers used many compounds, for example, tert-Butyl 4-carbamothioylpiperidine-1-carboxylate (cas: 214834-18-1Electric Literature of C11H20N2O2S).
tert-Butyl 4-carbamothioylpiperidine-1-carboxylate (cas: 214834-18-1) belongs to pyridine derivatives. The ring atoms in the pyridine molecule are sp2-hybridized. The nitrogen is involved in the π-bonding aromatic system using its unhybridized p orbital. The lone pair is in an sp2 orbital, projecting outward from the ring in the same plane as the σ bonds. Several pyridine derivatives play important roles in biological systems. While its biosynthesis is not fully understood, nicotinic acid (vitamin B3) occurs in some bacteria, fungi, and mammals.Electric Literature of C11H20N2O2S