Dubowchik, Gene M.; Michne, Jodi A.; Zuev, Dmitry; Schwartz, Wendy; Scola, Paul M.; James, Clint A.; Ruediger, Edward H.; Pin, Sokhom S.; Burris, Kevin D.; Balanda, Lynn A.; Gao, Qi; Wu, Dedong; Fung, Lawrence; Fiedler, Tracey; Browman, Kaitlin E.; Taber, Matthew T.; Zhang, Jie published the artcile< 2-Arylaminothiazoles as high-affinity corticotropin-Releasing factor 1 receptor (CRF1R) antagonists: synthesis, binding studies and behavioral efficacy>, Electric Literature of 112-63-0, the main research area is antidepressant thiazolemethanamine thiazolecarboxamide cyclopropylmethyl propyl preparation; structure activity antidepressant anxiolytic thiazolemethanamine thiazolecarboxamide cyclopropylmethyl propyl preparation; anxiolytic thiazolemethanamine thiazolecarboxamide cyclopropylmethyl propyl preparation; corticotropin releasing factor receptor thiazolemethanamine thiazolecarboxamide cyclopropylmethyl propyl preparation; human antidepressant thiazolemethanamine thiazolecarboxamide cyclopropylmethyl propyl preparation.
2-Arylamino-4-trifluoromethyl-5-aminomethylthiazoles represent a novel series of high-affinity corticotropin releasing factor-1 receptor (CRF1R) antagonists that are prepared in three steps in good overall yields. Herein, binding SAR as well as anxiolytic activity of an exemplary compound, N-(cyclopropylmethyl)-N-propyl-2-[(2,4,6-trichlorophenyl)amino]-4-(trifluoromethyl)-5-thiazolemethanamine (I), in a mouse canopy model were reported. Other compounds thus prepared and tested included N-(cyclopropylmethyl)-4-methyl-N-propyl-2-[(2,4,6-trichlorophenyl)amino]-5-thiazolecarboxamide, N,N-bis(2-methoxyethyl)-4-methyl-2-[(2,4,6-trichlorophenyl)amino]-5-thiazolecarboxamide, 2-[(2-chloro-4,6-dimethylphenyl)methylamino]-N-(cyclopropylmethyl)-N-propyl-4-(trifluoromethyl)-5-thiazolemethanamine, 2-[(2-chloro-4,6-dimethylphenyl)amino]-N-(cyclopropylmethyl)-N-propyl-4-(trifluoromethyl)-5-thiazolemethanamine. The activity of I was compared to that of an analog, N-(cyclopropylmethyl)-N-propyl-2-[(2,4,6-trichlorophenyl)amino]-4-(trifluoromethyl)-5-oxazolemethanamine.
Bioorganic & Medicinal Chemistry Letters published new progress about Antidepressants. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Electric Literature of 112-63-0.
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