title: Discovery of indolyl acrylamide derivatives as human diacylglycerol acyltransferase-2 selective inhibitors.
abstract: A series of indolyl acrylamide derivatives was synthesized as potential diacylglycerol acyltransferase (DGAT) inhibitors. Furfurylamine containing indolyl acrylamide derivative 5h exhibited the most potent DGAT inhibitory activity using microsomes prepared from rat liver. Further evaluation against human DGAT-1 and DGAT-2 identified indolyl acrylamide analogues as selective inhibitors against human DGAT-2. In addition, the most potent compound 5h inhibited triglyceride synthesis dose-dependently in HepG2 cell lines.
authors.affiliation: College of Pharmacy, Dongguk University-Seoul, Seoul 100-715, Korea.
authors.forename: Kyeong
authors.initials: K
authors.lastname: Lee
authors.forename: Minkyoung
authors.initials: M
authors.lastname: Kim
authors.forename: Boah
authors.initials: B
authors.lastname: Lee
authors.forename: Jail
authors.initials: J
authors.lastname: Goo
authors.forename: Jiyoung
authors.initials: J
authors.lastname: Kim
authors.forename: Ravi
authors.initials: R
authors.lastname: Naik
authors.forename: Jee Hee
authors.initials: JH
authors.lastname: Seo
authors.forename: Mun Ock
authors.initials: MO
authors.lastname: Kim
authors.forename: Youngjoo
authors.initials: Y
authors.lastname: Byun
authors.forename: Gyu-Yong
authors.initials: GY
authors.lastname: Song
authors.forename: Hyun Sun
authors.initials: HS
authors.lastname: Lee
authors.forename: Yongseok
authors.initials: Y
authors.lastname: Choi
mesh_terms: D020106:Acrylamide / Q000737:chemistry* / Q000494:pharmacology*; D000818:Animals; D051048:Diacylglycerol O-Acyltransferase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D056945:Hep G2 Cells; D006801:Humans; D008861:Microsomes / Q000187:drug effects / Q000378:metabolism; D051381:Rats; D014280:Triglycerides / Q000037:antagonists & inhibitors / Q000378:metabolism
chemical_list: D014280:Triglycerides; D020106:Acrylamide; C494885:DGAT2 protein, human; D051048:Diacylglycerol O-Acyltransferase