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- …

…, H Tanaka, A Ohoka-Sugita, F Io, H Koretsune…

Index: Chonan, Tomomichi; Wakasugi, Daisuke; Yamamoto, Daisuke; Yashiro, Miyoko; Oi, Takahiro; Tanaka, Hiroaki; Ohoka-Sugita, Ayumi; Io, Fusayo; Koretsune, Hiroko; Hiratate, Akira Bioorganic and Medicinal Chemistry, 2011 , vol. 19, # 5 p. 1580 - 1593

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Citation Number: 15

Abstract

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 ...