940933-23-3Relevant articles and documents
Discovery of novel (4-piperidinyl)-piperazines as potent and orally active acetyl-CoA carboxylase 1/2 non-selective inhibitors: F-Boc and triF-Boc groups are acid-stable bioisosteres for the Boc group
Chonan, Tomomichi,Wakasugi, Daisuke,Yamamoto, Daisuke,Yashiro, Miyoko,Oi, Takahiro,Tanaka, Hiroaki,Ohoka-Sugita, Ayumi,Io, Fusayo,Koretsune, Hiroko,Hiratate, Akira
, p. 1580 - 1593 (2011)
Novel (4-piperidinyl)-piperazine derivatives were synthesized and evaluated as ACC1/2 non-selective inhibitors. Optimization of the substituents on the nitrogen of the piperidine ring led to the identification of the fluorine substituted tert-butoxycarbonyl group. Advanced analog, 1,1,1-trifluoro-2- methylpropan-2-yl 4-{4-[(2-amino-6-methyl-1-benzothiophen-3-yl)carbonyl] piperazin-1-yl}piperidine-1-carboxylate (12c) showed potent inhibitory activities in enzyme-assay and cell-based assays. Compound 12c also exhibited reduction of hepatic de novo fatty acid synthesis in rats after oral administration.