A novel class of apical sodium-dependent bile acid transporter inhibitors: the amphiphilic 4-oxo-1-phenyl-1,4-dihydroquinoline derivatives.
A series of 4-oxo-1-phenyl-1,4-dihydroquinolines possessing a linker and an ammonio moiety were synthesized and found to inhibit the apical sodium-dependent bile acid transporter (ASBT). The potency of ASBT inhibition varied with the position and length of the linking tether. Compound 21e effectively lowered the total serum cholesterol levels in hamsters.
Kurata
Hitoshi
H
Research Laboratories, Sankyo Co. Ltd, Hiromachi, Shinagawa-ku, Tokyo 140-8710, Japan. hitosi@shina.sankyo.co.jp
Suzuki
Sayaka
S
Ohhata
Yasuo
Y
Ikeda
Takuya
T
Hasegawa
Toru
T
Kitayama
Ken
K
Inaba
Toshimori
T
Kono
Keita
K
Kohama
Takafumi
T
D000818:Animals; D000924:Anticholesteremic Agents / Q000737:chemistry / Q000494:pharmacology; D002784:Cholesterol / Q000097:blood; D006224:Cricetinae; D008297:Male; D008647:Mesocricetus; D029363:Organic Anion Transporters, Sodium-Dependent / Q000037:antagonists & inhibitors* / Q000378:metabolism; D011804:Quinolines / Q000737:chemistry* / Q000494:pharmacology*; D027981:Symporters / Q000037:antagonists & inhibitors* / Q000378:metabolism
D000924:Anticholesteremic Agents; D029363:Organic Anion Transporters, Sodium-Dependent; D011804:Quinolines; D027981:Symporters; C071908:sodium-bile acid cotransporter; D002784:Cholesterol