Document Report Card

ID: ALA1124322

Journal: J Med Chem

Title: Synthesis and alpha 2-adrenoceptor antagonist activity of some disulfonamidobenzoquinolizines.

Authors: Ward TJ, Warrellow GJ, Stirrup JA, Lattimer N, Rhodes KF.

Abstract: A series of disulfonamidobenzo[a]quinolizines were synthesized and evaluated for their alpha 2- and alpha 1-adrenoceptor antagonist activity on the rat vas deferens and anococcygeus muscle, respectively. N-((2 beta,11b alpha)-1,3,4,6,7,11b-Hexahydro-2H-benzo[a]quinolizin-2-yl)-N- [2-[(methylsulfonyl)amino]ethyl]methanesulfonamide (4) and its N-[2-[(methylsulfonyl)amino]ethyl]ethanesulfonamide (22), N-[2-[(ethylsulfonyl)amino]ethyl]ethanesulfonamide (27), and N-[2-[(methylsulfonyl)amino]ethyl]-4-methylbenzenesulfonamide (30) analogues showed 400-fold or greater selectivity in favor of alpha 2- over alpha 1-adrenoceptor blockade.

CiteXplore: 2562854

DOI: 10.1021/jm00121a033