Design of a novel class of biphenyl CETP inhibitors.
A new class of CETP inhibitors was designed and prepared. These compounds are potent both in vitro and in vivo. The most active compound (12d) has shown an ability to raise HDL significantly in transgenic mouse PD model.
Department of Medicinal Chemistry, Merck Sharp & Dohme Corp., Rahway, NJ 07065, USA. zhijian_lu@merck.com
Zhijian
Z
Lu
Joann B
JB
Napolitano
Ashleigh
A
Theberge
Amjad
A
Ali
Milton L
ML
Hammond
Eugene
E
Tan
Xinchun
X
Tong
Suoyu S
SS
Xu
Melanie J
MJ
Latham
Laurence B
LB
Peterson
Matt S
MS
Anderson
Suzanne S
SS
Eveland
Qiu
Q
Guo
Sheryl A
SA
Hyland
Denise P
DP
Milot
Ying
Y
Chen
Carl P
CP
Sparrow
Samuel D
SD
Wright
Peter J
PJ
Sinclair
D000818:Animals; D001596:Benzylamines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D001713:Biphenyl Compounds / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D002219:Carbamates / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D053480:Cholesterol Ester Transfer Proteins / Q000037:antagonists & inhibitors* / Q000378:metabolism; D004195:Disease Models, Animal; D015195:Drug Design; D008075:Lipoproteins, HDL / Q000378:metabolism; D051379:Mice; D008822:Mice, Transgenic; D013329:Structure-Activity Relationship
D001596:Benzylamines; D001713:Biphenyl Compounds; D002219:Carbamates; D053480:Cholesterol Ester Transfer Proteins; D008075:Lipoproteins, HDL; C010574:biphenyl