Saito, Tetsuji; Obitsu, Tetsuo; Minamoto, Chiaki; Sugiura, Tsuneyuki; Matsumura, Naoya; Ueno, Sonoko; Kishi, Akihiro; Katsumata, Seishi; Nakai, Hisao; Toda, Masa-Aki published the artcile< Pyrazolo[1,5-a]pyrimidines, triazolo[1,5-a]pyrimidines and their tricyclic derivatives as corticotropin-releasing factor 1 (CRF1) receptor antagonists>, Safety of 4-Chloro-2-(methylthio)pyrazolo[1,5-a][1,3,5]triazine, the main research area is pyrazolopyrimidine triazolopyrimidine preparation corticotropin releasing factor receptor antagonist; structure activity relationship CRF receptor antagonist pyrazolopyrimidine triazolopyrimidine.
To identify structurally novel CRF1 receptor antagonists, a series of bicyclic core antagonists, pyrazolo[1,5-a]pyrimidines, e.g. I (X = CH), triazolo[1,5-a]pyrimidines, e.g. I (X = N), imidazo[1,2-a]pyrimidines, e.g. II, and a pyrazolo[1,5-a][1,3,5]triazine, III, were designed, synthesized and evaluated as CRF1 receptor antagonists. Several compounds showed binding affinity (IC50 = 4.2-418 nM) and antagonist activity (EC50 = 4.0-889 nM). Compound I (X = CH) was found to show oral efficacy in an Elevated Plus Maze test in rats. Further chem. modification of them led us to discovery of the tricyclic core antagonists pyrazolo[1,5-a]pyrrolo[3,2-e]pyrimidines, e.g. IV. The discovery process of these compounds is presented, as is the study of the structure-activity relationship.
Bioorganic & Medicinal Chemistry published new progress about Aromatic amines Role: RCT (Reactant), RACT (Reactant or Reagent). 54346-19-9 belongs to class pyrazoles-derivatives, and the molecular formula is C6H5ClN4S, Safety of 4-Chloro-2-(methylthio)pyrazolo[1,5-a][1,3,5]triazine.
Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics