Journal of Medicinal Chemistry p. 1426 - 1433 (1983)
Update date:2022-08-02
Topics:
Caroon, Joan M.
Clark, Robin D.
Kluge, Arthur F.
Lee, Chi-Ho
Strosberg, Arthur M.
The 2R*,11bS* and 2S*,11bS* diastereoisomers of the spiro<1,3,4,6,7,11b-hexahydro-2H-benzoquinolizine-2,5'-oxazolidin-2'-one> system were prepared by stereoselective methods.Evaluation of these compounds for antihypertensive activity by oral administration to the spontaneously hypertensive rat showed the 2S*,11bS* series was the more potent.Within that series it was found that small alkyl substituents at positions 3 and 4' enhanced antihypertensive activity and that methoxyl substitution at positions 9 and 10 was optical. (2S,3S,11bS)-Spiro<2-ethyl-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-benzoquinolizine-2,5'-oxazolidin-2'-one> <(-)-9e> was one of the most efficacious compounds of this series, while its antipode, (+)-9e, was inactive.Selected compounds in this series were shown to be α-adrenoceptor antagonists.
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