147962-81-0Relevant articles and documents
Smo inhibitor as well as synthesis method and application thereof
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Paragraph 0044; 0045; 0048-0051, (2019/09/17)
The invention discloses an Smo inhibitor as well as a synthesis method and application thereof. A structural formula of the Smo inhibitor is shown by a formula (I) as shown in the specification. The invention also discloses the synthesis method and the application of the Smo inhibitor. According to the invention, nilotinib is optimized into the dual-targeted inhibitor being active against Smo andBcr-Abl, and the inhibitor can overcome the tolerance problem caused by single-targeted drugs, has the advantages of improving anti-tumor efficacy and reducing toxic or side effects, and provides a reference for future research on dual-targeted anti-hematologic malignant drugs.
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
experimental part, p. 3005 - 3021 (2011/06/19)
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.
Benzimidazol-2-yl or benzimidazol-2-ylthiomethyl benzoylguanidines as novel Na+/H+ exchanger inhibitors, synthesis and protection against ischemic-reperfusion injury
Zhang, Rui,Lei, Lin,Xu, Yun-Gen,Hua, Wei-Yi,Gong, Guo-Qing
, p. 2430 - 2433 (2008/04/18)
A novel series of benzimidazol-2-yl or benzimidazol-2-ylthiomethyl benzoylguanidines were designed and synthesized as Na+/H+exchanger inhibitors. Most of them were found to inhibit NHE1-mediated platelet swelling in a concentration-dependent manner, and to have significant cardioprotective effect against myocardial ischemic-reperfusion injury, among which compounds 10a and 34 were more potent than cariporide in both in vivo and in vitro tests.