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Synthesis and α2-Adrenoceptor Antagonist Activity of Some Disulfonamidobenzoquinolizines

DOI: 10.1021/jm00121a033

Source and publish data:

Journal of Medicinal Chemistry p. 179 - 182 (1989)

Update date:2022-09-26

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Authors:

Ward, Terence J.Ward, Terence J.

Warrellow, Graham J.Warrellow, Graham J.

Stirrup, John A.Stirrup, John A.

Lattimer, NormanLattimer, Norman

Rhodes, Keith F.Rhodes, Keith F.

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Article abstract of DOI:10.1021/jm00121a033

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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Full text of DOI:10.1021/jm00121a033

Products guided by the article

Product name:N-(2-Ethanesulfonylamino-ethyl)-N-(2R,11bS)-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-yl-4-methyl-benzenesulfonamide; compound with (Z)-but-2-enedioic acid

Cas No:117145-32-1

117145-32-1

R&D Labs maybe for 117145-32-1

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