Journal of Medicinal Chemistry p. 179 - 182 (1989)
Update date:2022-09-26
Topics:
Ward, Terence J.
Warrellow, Graham J.
Stirrup, John A.
Lattimer, Norman
Rhodes, Keith F.
A series of disulfonamidobenzoquinolizines were synthesized and evaluated for their α2- and α1-adrenoceptor antagonist activity on the rat vas deferens and anococcygeus muscle, respectively.N-((2β,11bα)-1,3,4,6,7,11b-Hexahydro-2H-benzoquinolizin-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 α2- over α1-adrenoceptor blockade.
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