Stereochemical influences upon antihistamine activity. Further studies of isomeric 4-amino-1, 2-diarylbutenes
- 1 April 1970
- journal article
- Published by Oxford University Press (OUP) in Journal of Pharmacy and Pharmacology
- Vol. 22 (4) , 270-278
- https://doi.org/10.1111/j.2042-7158.1970.tb08518.x
Abstract
The acid-catalysed dehydration of some 4-amino-1, 2-diarylbutan-2-ols yields all four possible 4-amino-1, 2-diarylbutenes. The structure and configuration of pure isomers have been established from spectroscopic data, and the ability of these compounds to anatagonize histamine-induced contractions of the guinea-pig ileum is reported. The most potent derivatives are all cis(H/Ar)-4-amino-1, 2-diarylbut-2-enes. These results together with other data are discussed in terms of the possible structural and conformational requirements of histamine antagonists.Keywords
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