Piperidineacrylate derivatives as potential antiallergy agents.
A new series of piperidineacrylate derivatives was prepared and evaluated for antiallergic activity. Most of the compounds showed potent activities in the rat passive cutaneous anaphylaxis (PCA) assay. In particular, ethyl 1-[2-bis(4-fluorophenyl)methoxyethyl]-4-piperidineacrylate (1a) was more potent than oxatomide and terfenadine in this assay, and was selected for further study. Some pharmacological properties of 1a are presented.
Sugiyama
M
M
Medicinal Chemistry Research Laboratory, Sankyo Co., Ltd., Tokyo, Japan.
Sakamoto
T
T
Kamigaki
Y
Y
Fukumi
H
H
Itoh
K
K
Satoh
Y
Y
Yamaguchi
T
T
D000179:Acrylates / Q000138:chemical synthesis / Q000494:pharmacology; D000818:Animals; D006168:Guinea Pigs; D006967:Hypersensitivity / Q000188:drug therapy*; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D010323:Passive Cutaneous Anaphylaxis / Q000187:drug effects; D010880:Piperidines / Q000138:chemical synthesis* / Q000494:pharmacology*; D051381:Rats; D017207:Rats, Sprague-Dawley
D000179:Acrylates; D010880:Piperidines