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Benzo[b]thiophene-2-carboxamide Derivatives as Potent urotensin-II Receptor Antagonists

Benzo[b]thiophene-2-carboxamide Derivatives as Potent urotensin-II Receptor Antagonists

Chae Jo Lim, Seong Eun Woo, Su Ik Ko, Byung Ho Lee, Kwang-Seok Oh, Kyu Yang Yi

Bioorg Med Chem Lett. 2016 Oct 1;26(19):4684-4686.

PMID: 27597245

Abstract:

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 (R(1) and R(2)) 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 7f as a highly potent UT antagonist with an IC50 value of 25nM. Despite having a good metabolic stability, 7f is a potent inhibitor of CYP isozyme and displays an unsuitable PK profile.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP148961880	2-Tributylstannylbenzo[b]thiophene		148961-88-0	Price

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