A novel class of apical sodium co-dependent bile acid transporter inhibitors: the 2,3-disubstituted-4-phenylquinolines.
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.
Tollefson
M B
MB
Searle Discovery, Monsanto Life Sciences, St. Louis, MO 63198, USA.
Vernier
W F
WF
Huang
H C
HC
Chen
F P
FP
Reinhard
E J
EJ
Beaudry
J
J
Keller
B T
BT
Reitz
D B
DB
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)
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)