title: Piperidineacrylate derivatives as potential antiallergy agents.
abstract: 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.
authors.affiliation: Medicinal Chemistry Research Laboratory, Sankyo Co., Ltd., Tokyo, Japan.
authors.forename: M
authors.initials: M
authors.lastname: Sugiyama
authors.forename: T
authors.initials: T
authors.lastname: Sakamoto
authors.forename: Y
authors.initials: Y
authors.lastname: Kamigaki
authors.forename: H
authors.initials: H
authors.lastname: Fukumi
authors.forename: K
authors.initials: K
authors.lastname: Itoh
authors.forename: Y
authors.initials: Y
authors.lastname: Satoh
authors.forename: T
authors.initials: T
authors.lastname: Yamaguchi
mesh_terms: 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
chemical_list: D000179:Acrylates; D010880:Piperidines