PROSTAGLANDIN-ACETYLENE ANALOGUES

摘要

Optically active and racemic prostaglandin derivatives of the formula wherein R1 is -OR5; -NHSO2CH3; or -O-CH2-U-V; R5 is hydrogen, alkyl, aryl, or a heterocyclic group; U is a direct bond, carbonyl or carbonyloxy; and V is phenyl substituted by 1-3 phenyl, alkoxy of 1-2 carbon atoms, or halogen, preferably bromine; R2 is hydrogen or alkyl of 1-5 carbon atoms; R3 is alkyl, substituted or unsubstituted cycloalkyl, straight-chain or branched alkyl of 1-5 carbon atoms substituted by aryl or substituted aryl, when R1 is as above; or R3 is aryl or substituted aryl group when R1 is -OR5', -NHSO2CH3, or -O-CH2-U-V and R5' is aryl or a heterocyclic group and U and V are as above; R4 is hydrogen or an ether or acyl residue; A is -CH2-CH2- or cis-CH=CH-; B is -CH2-CH2- or trans-CH=CH-; D is a direct bond, oxygen, or sulfur; Z is carbonyl or >CH OR4 wherein OR4 is in the alpha - or beta -position; and X Y is when Z is >CH OR4-, or or -CH=CH- when Z is carbonyl; AND, WHEN R1 is hydroxy, the physiologically compatible salts thereof with bases, have more prolonged activity than naturally-occurring prostaglandins.