Benzo[b]thiophene-2-carboxamide derivatives as potent urotensin-II receptor antagonists was written by Lim, Chae Jo;Woo, Seong Eun;Ko, Su Ik;Lee, Byung Ho;Oh, Kwang-Seok;Yi, Kyu Yang. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2016.Application of 7312-11-0 This article mentions the following:
Members of a series of benzo[b]thiophene-2-carboxamide derivatives, possessing an N-(1-(3-bromo-4-(piperidin-4-yloxy)benzyl)piperidin-4-yl) group, were synthesized and evaluated as urotensin-II receptor antagonists. The results show that these substances have potent UT binding affinities. Observations made in a systematic SAR investigation of the effects of a variety of substituents at the 5- and 6-positions in the benzo[b]thiophene-2-carboxamide moiety on UT binding affinities led to identification of the 5-cyano analog I as a highly potent UT antagonist with an IC50 value of 25 nM. Despite having a good metabolic stability, compound I is a potent inhibitor of CYP isoenzyme and displays an unsuitable PK profile. In the experiment, the researchers used many compounds, for example, Methyl 5-bromobenzo[b]thiophene-2-carboxylate (cas: 7312-11-0Application of 7312-11-0).
Methyl 5-bromobenzo[b]thiophene-2-carboxylate (cas: 7312-11-0) belongs to benzothiophene derivatives. Benzothiophene is relatively a stable molecule. The electrophilic substitution of benzothiophene systems is much less regioselective than that of indoles. It has been used as a raw material for the synthesis of biologically active structures and is found in pharmaceuticals such as leukotriene synthesis inhibitors and antifungals, as well as in many natural products.Application of 7312-11-0
Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem