Sugiyama M, Sakamoto T, Kamigaki Y, Fukumi H, Itoh K, Satoh Y, Yamaguchi T
Medicinal Chemistry Research Laboratory, Sankyo Co., Ltd., Tokyo, Japan.
Chem Pharm Bull (Tokyo). 1993 May;41(5):882-8. doi: 10.1248/cpb.41.882.
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.