|
|||||
|
|
Potent antagonists of the Kv1.5 potassium channel: synthesis and evaluation of analogous N,N-diisopropyl-2-(pyridine-3-yl)acetamides |
|
| Authors: | Nanda Kausik K Nolt M Brad Cato Matthew J Kane Stefanie A Kiss Laszlo Spencer Robert H Wang Jixin Lynch Joseph J Regan Christopher P Stump Gary L Li Bing White Rebecca Yeh Suzie Bogusky Michael J Bilodeau Mark T Dinsmore Christopher J Lindsley Craig W Hartman George D Wolkenberg Scott E Trotter B Wesley |
| Affiliation: | Department of Medicinal Chemistry, Merck Research Laboratories, Merck and Co., Inc., PO Box 4, West Point, PA 19486, USA. |
| Abstract: | This letter describes the discovery of a novel series of potent Kv1.5 ion channel antagonists based on a diisopropyl amide scaffold. Structure-activity relationships of functionalized analogs are discussed. Key compound 1-(3-(diisopropylcarbamoyl)-2-phenyl-3-(pyridin-3-yl)propyl)-3-(2-fluorobenzyl)urea (10) exhibits significant atrial-selective effects in an in vivo model. |
| Keywords: | |
| 本文献已被 ScienceDirect PubMed 等数据库收录！ | |