Abstract:
:Novel analogues of the class III antiarrhythmic agent 1-[2-hydroxy-2-[4-[(methylsulfonyl)amino]phenyl]ethyl]-3-methyl-1H- imidazolium chloride, 1 (CK-1649), were prepared and investigated for their class III electrophysiological activity on isolated canine cardiac Purkinje fibers and ventricular muscle tissue. Structure-activity relationships are discussed for a series of 11 compounds. One compound, N-[4-[1-hydroxy-2-(4,5-dihydro-2-methyl-1H-imidazol-1- yl)ethyl]phenyl]methanesulfonamide hydrochloride, 9, was comparable in activity to 1 in vitro and prolonged the functional refractory period in anesthetized dogs when given intraduodenally. Unlike 1, compound 9 was ineffective at preventing ventricular tachycardia induced by programmed electrical stimulation in anesthetized dogs 24 h after an acute myocardial infarction.
journal_name
J Med Chemjournal_title
Journal of medicinal chemistryauthors
Lis R,Davey DD,Morgan TK Jr,Lumma WC Jr,Wohl RA,Jain VK,Wan CN,Argentieri TM,Sullivan ME,Cantor EHdoi
10.1021/jm00395a021subject
Has Abstractpub_date
1987-12-01 00:00:00pages
2303-9issue
12eissn
0022-2623issn
1520-4804journal_volume
30pub_type
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