2-Arylbenzoxazoles as CETP inhibitors: Substitution of the benzoxazole moiety.
A series of 2-arylbenzoxazole inhibitors of the cholesterol ester transfer protein (CETP) is described. Structure-activity studies focused on variation of the substitution of the benzoxazole moiety. Substitution at the 5- and 7-positions of the benzoxazole moiety was found to be beneficial for CETP inhibition. Compound 47 was found to be the most potent inhibitor in this series and inhibited CETP with an IC(50) of 28nM.
Smith
Cameron J
CJ
Department of Medicinal Chemistry, Merck Research Laboratories, Rahway NJ 07065, United States. cameron_smith@merck.com
Ali
Amjad
A
Chen
Liya
L
Hammond
Milton L
ML
Anderson
Matt S
MS
Chen
Ying
Y
Eveland
Suzanne S
SS
Guo
Qiu
Q
Hyland
Sheryl A
SA
Milot
Denise P
DP
Sparrow
Carl P
CP
Wright
Samuel D
SD
Sinclair
Peter J
PJ
D000083:Acetanilides / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D000284:Administration, Oral; D000818:Animals; D000924:Anticholesteremic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D001583:Benzoxazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D053480:Cholesterol Ester Transfer Proteins / Q000037:antagonists & inhibitors* / Q000378:metabolism; D051379:Mice; D013329:Structure-Activity Relationship
D000083:Acetanilides; D000924:Anticholesteremic Agents; D001583:Benzoxazoles; D053480:Cholesterol Ester Transfer Proteins