title: A novel class of apical sodium co-dependent bile acid transporter inhibitors: the 2,3-disubstituted-4-phenylquinolines.
abstract: A series of 2,3-disubstituted-4-phenylquinolines were prepared and were found to inhibit the apical sodium co-dependent bile acid transporter (ASBT). Alkyl and ester substitution at the 3-position showed comparable activities while substitution at the 2-position was much more sensitive to the nature of the substituent. The synthesis and in vitro potency data are presented for this novel class of compounds.
authors.affiliation: Searle Discovery, Monsanto Life Sciences, St. Louis, MO 63198, USA.
authors.forename: M B
authors.initials: MB
authors.lastname: Tollefson
authors.forename: W F
authors.initials: WF
authors.lastname: Vernier
authors.forename: H C
authors.initials: HC
authors.lastname: Huang
authors.forename: F P
authors.initials: FP
authors.lastname: Chen
authors.forename: E J
authors.initials: EJ
authors.lastname: Reinhard
authors.forename: J
authors.initials: J
authors.lastname: Beaudry
authors.forename: B T
authors.initials: BT
authors.lastname: Keller
authors.forename: D B
authors.initials: DB
authors.lastname: Reitz
mesh_terms: D002352:Carrier Proteins / Q000037:antagonists & inhibitors*; D006913:Hydroxysteroid Dehydrogenases; D008562:Membrane Glycoproteins; D015394:Molecular Structure; D011804:Quinolines / Q000737:chemistry / Q000494:pharmacology*; D012964:Sodium / Q000494:pharmacology*; D045002:3-alpha-Hydroxysteroid Dehydrogenase (B-Specific)
chemical_list: D002352:Carrier Proteins; D006913:Hydroxysteroid Dehydrogenases; D008562:Membrane Glycoproteins; D011804:Quinolines; D012964:Sodium; C037643:bile acid binding proteins; C435496:AKR1C2 protein, human; D045002:3-alpha-Hydroxysteroid Dehydrogenase (B-Specific)