Imidazopyridine-Based Fatty Acid Synthase Inhibitors That Show Anti-HCV Activity and in Vivo Target Modulation

Johan D Oslob; Russell J Johnson; Haiying Cai; Shirley Q Feng; Lily Hu; Yuko Kosaka; Julie Lai; Mohanram Sivaraja; Samnang Tep; Hanbiao Yang; Cristiana A Zaharia; Marc J Evanchik; Robert S McDowell

doi:10.1021/ml300335r

Imidazopyridine-Based Fatty Acid Synthase Inhibitors That Show Anti-HCV Activity and in Vivo Target Modulation

ACS Med Chem Lett. 2012 Dec 2;4(1):113-7. doi: 10.1021/ml300335r. eCollection 2013 Jan 10.

Affiliation

¹ 3-V Biosciences, Inc. , 1050 Hamilton Court, Menlo Park, California 94025, United States.

Abstract

Potent imidazopyridine-based inhibitors of fatty acid synthase (FASN) are described. The compounds are shown to have antiviral (HCV replicon) activities that track with their biochemical activities. The most potent analogue (compound 19) also inhibits rat FASN and inhibits de novo palmitate synthesis in vitro (cell-based) as well as in vivo.

Keywords: FASN; HCV; antiviral; in vivo; inhibitor; reversible; structure−activity relationship; target modulation.