Dow, Robert L. published the artcileDiscovery of 2-(2-Chlorophenyl)-3-(4-chlorophenyl)-7-(2,2-difluoropropyl)-6,7-dihydro-2H-pyrazolo[3,4-f][1,4]oxazepin-8(5H)-one (PF-514273), a Novel, Bicyclic Lactam-Based Cannabinoid-1 Receptor Antagonist for the Treatment of Obesity, SDS of cas: 371-99-3, the publication is Journal of Medicinal Chemistry (2009), 52(9), 2652-2655, database is CAplus and MEDLINE.
The design, synthesis, and structure-activity relationships of novel bicyclic lactams I (R1 = 2-ClC6H4; R2 = 4-ClC6H4; R3 = H, Et, i-Pr, i-Bu, cyclopentyl, CH2CF2Me, etc.) and II (R4 = H, i-Pr, CH2CF3, CH2CF2Me, CH2CF2Et) as cannabinoid type 1 (CB1) receptor antagonists is described. Members of these series are potent, selective antagonists in in vitro/in vivo efficacy models of CB1 antagonism and exhibit robust oral activity in rodent models of food intake. These efforts led to the identification of II (R4 = CH2CF2Me), which has been advanced to human clin. trials for weight management.
Journal of Medicinal Chemistry published new progress about 371-99-3. 371-99-3 belongs to alcohols-buliding-blocks, auxiliary class Trifluoromethylated Building Blocks, name is 2-((2,2,2-Trifluoroethyl)amino)ethanol, and the molecular formula is C4H8F3NO, SDS of cas: 371-99-3.
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