943783-97-9Relevant academic research and scientific papers
Synthesis and structure-activity relationship of tricyclic carboxylic acids as novel anti-histamines
Kubota, Katsumi,Kurebayashi, Hirotaka,Miyachi, Hirotaka,Tobe, Masanori,Onishi, Masako,Isobe, Yoshiaki
, p. 3005 - 3021 (2011)
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-induced biphasic cutaneous reaction model. Among the compounds tested, dibenzoxazepine carboxylic acid 13b showed both histamine H1 receptor antagonistic activity and anti-inflammatory activity in vivo. In addition, 13b exhibited low affinity toward α1 receptor and low occupancy of H1 receptor in the brain. It is therefore, believed that 13b is a potential candidate for development as 3rd generation anti-histamine.
