Synthesis and preliminary pharmacological evaluation of asymmetric chloroquine analogs

…, DA Grattan, RJ Heaslip, RG Rahwan

Index: Witiak, Donald T.; Grattan, David A.; Heaslip, Richard J.; Rahwan, Ralf G. Journal of Medicinal Chemistry, 1981 , vol. 24, # 6 p. 712 - 717

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Citation Number: 5

Abstract

Asymmetric chloroquine analogues (1-4) were prepared of known absolute configuration in order to assess stereochemical influences on selected biological activities. Since chloroquine has been shown to possess spasmolytic properties, analogues 1-4 were tested for similar pharmacological effects on smooth-muscle contraction. The (S)-and (R)- chlorochloroquine enantiomers (1 and 2, respectively) were more potent antispasmodics ...