Referenced in: none

Automatically associated channels: Kv11.1

Title: Synthesis and SAR of thieno[3,2-b]pyridinyl urea derivatives as urotensin-II receptor antagonists.

Authors: Chae Jo Lim, Seung Ae Oh, Byung Ho Lee, Kwang-Seok Oh, Kyu Yang Yi

Journal, date & volume: Bioorg. Med. Chem. Lett., 2014 Dec 15 , 24, 5832-5

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/25452001

Abstract
The preparation and SAR profile of thieno[3,2-b]pyridinyl urea derivatives as novel and potent urotensin-II receptor antagonists are described. An activity optimization study, probing the effects of substituents on thieno[3,2-b]pyridinyl core and benzyl group of the piperidinyl moiety, led to the identification of p-fluorobenzyl substituted thieno[3,2-b]pyridinyl urea 6n as a highly potent UT antagonist with an IC50 value of 13nM. Although 6n displays good metabolic stability and low hERG binding activity, it has an unacceptable oral bioavailability.