78706-26-0Relevant articles and documents
BCL6-targeting aromatic ring five-membered aromatic heterocyclic micromolecular organic compound and derivative and application thereof
-
Paragraph 0171-0173; 0175, (2021/03/24)
The invention discloses an aromatic ring five-membered aromatic heterocyclic micromolecular organic compound or related analogues or pharmaceutically acceptable salts thereof. The structures of the compound are shown as formulas (I-IX). The invention also
The identification of GPR3 inverse agonist AF64394; The first small molecule inhibitor of GPR3 receptor function
Jensen, Thomas,Elster, Lisbeth,Nielsen, Soren Moller,Poda, Suresh Babu,Loechel, Frosty,Volbracht, Christiane,Klewe, Ib Vestergaard,David, Laurent,Watson, Stephen P.
, p. 5195 - 5198 (2014/12/11)
The identification of the novel and selective GPR3 inverse agonist AF64394, the first small molecule inhibitor of GPR3 receptor function, is described. Structure activity relationships and syntheses based around AF64394 are reported.
Pyrazolo[1,5-a]pyrimidines, triazolo[1,5-a]pyrimidines and their tricyclic derivatives as corticotropin-releasing factor 1 (CRF1) receptor antagonists
Saito, Tetsuji,Obitsu, Tetsuo,Minamoto, Chiaki,Sugiura, Tsuneyuki,Matsumura, Naoya,Ueno, Sonoko,Kishi, Akihiro,Katsumata, Seishi,Nakai, Hisao,Toda, Masaaki
scheme or table, p. 5955 - 5966 (2011/11/04)
To identify structurally novel CRF1 receptor antagonists, a series of bicyclic core antagonists, pyrazolo[1,5-a]pyrimidines, triazolo[1,5-a] pyrimidines, imidazo[1,2-a]pyrimidines and pyrazolo[1,5-a][1,3,5]triazines were designed, synthesized and evaluated as CRF1 receptor antagonists. Compounds 2-27 showed binding affinity (IC50 = 4.2-418 nM) and antagonist activity (EC50 = 4.0-889 nM). Compound 5 was found to show oral efficacy in an Elevated Plus Maze test in rats. Further chemical modification of them led us to discovery of the tricyclic core antagonists pyrazolo[1,5-a]pyrrolo[3,2-e] pyrimidines. The discovery process of these compounds is presented, as is the study of the structure-activity relationship.