86457-40-1Relevant articles and documents
Synthesis and Antihypertensive Activity of a Series of Spiroquinolizine-2,5'-oxazolidin-2'-one>s
Caroon, Joan M.,Clark, Robin D.,Kluge, Arthur F.,Lee, Chi-Ho,Strosberg, Arthur M.
, p. 1426 - 1433 (2007/10/02)
The 2R*,11bS* and 2S*,11bS* diastereoisomers of the spiroquinolizine-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)-Spiroquinolizine-2,5'-oxazolidin-2'-one> 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.