Journal of Medicinal Chemistry p. 2238 - 2243 (1992)
Update date:2022-09-26
Topics:
Rose, Ulrich
Draeger, Martin
Enantiomerically pure hexahydroquinolinones of the structural type 9 were prepared by a variation of the Hantzsch synthesis in which an optically active acetoacetate served as a chiral auxiliary reagent.Determination of the de and ee values are described.The absolute configurations of the optically pure products were characterized by single-crystal X-ray analysis.The antipodes 9a and 9b exhibited calcium antagonistic activities on smooth musculature; the (S)-(-)-enantiomer 9b was the more potent compound with regard to the EC50 values which differed by a factor of 100; the intrinsic axctivity of 9b was 1.2, compared with a value of 0.54 for 9a.On the other hand, R-(+)-9a exerted positive inotropic effects on electrically stimulated atria.The cause of these effects is discussed.
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