학술논문
Design and Synthesis of 4-Substituted Benzamides as Potent, Selective, and Orally Bioavailable IKs Blockers
Document Type
Article
Author
Source
Journal of Medicinal Chemistry; November 2001, Vol. 44 Issue: 23 p3764-3767, 4p
Subject
Language
ISSN
00222623; 15204804
Abstract
Multiple delayed rectifier potassium currents, including IKs , are responsible for the repolarization and termination of the cardiac action potential, and blockers of these currents may be useful as antiarrhythmic agents. Modification of compound 5 produced 19(S) that is the most potent IKs blocker reported to date with >5000-fold selectivity over other cardiac ion channels. Further modification produced 24A with 23% oral bioavailability.