Synthesis and structure–activity relationship of tricyclic carboxylic acids as novel anti-histamines

K Kubota, H Kurebayashi, H Miyachi, M Tobe…

文献索引：Kubota, Katsumi; Kurebayashi, Hirotaka; Miyachi, Hirotaka; Tobe, Masanori; Onishi, Masako; Isobe, Yoshiaki Bioorganic and Medicinal Chemistry, 2011 , vol. 19, # 9 p. 3005 - 3021

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被引用次数: 13

摘要

Abstract A series of tricyclic carboxylic acids having 6-amino-pyrimidine-2, 4 (1H, 3H)-dione with piperazino or homopiperazino moiety linked by propylene, were synthesized and evaluated for their affinity toward human histamine H 1 receptor and Caco-2 cell permeability. Selected compounds were further evaluated for their oral anti-histaminic activity in mice, bioavailability in rats, and their anti-inflammatory activity in mice OVA- ...