Butyrophenones as hypotensive agents. Derivatives of 4-aryl-4-(hydroxymethyl)cyclohexylamine.

Autor: Lednicer D, Emmert ED, Rudzik AD, Graham BE
Jazyk: angličtina
Zdroj: Journal of medicinal chemistry [J Med Chem] 1975 Jun; Vol. 18 (6), pp. 593-9.
DOI: 10.1021/jm00240a014
Abstrakt: The preparation of butyrophenone derivatives of 4-aryl-4-(hydroxymethyl)cyclohex-1-ylamines starting from the corresponding 4-cyano-4-phenylcyclohexan-1-ones is described. Substitution was varied with both rings; both isomers of 4-phenyl-4-(hydroxymethyl)cyclohex-1-ylamine were characterized. Those derivatives which carried p-fluoro substitution on the butyrophenone exhibited hypotensive activity in the rat with diminished CNS activity compared to compounds lacking the hydroxymethyl group. The effect of substitution on the 4-aryl ring is discussed.
Databáze: MEDLINE