2-Arylbenzoxazoles as novel cholesteryl ester transfer protein inhibitors: optimization via array synthesis.
2-Arylbenzoxazole 5 was identified as a hit from a fluorescence-based high-throughput screen for CETP inhibitors. The synthesis and SAR investigation employing array synthesis of the A- and B-rings are described.
Harikrishnan
Lalgudi S
LS
Bristol-Myers Squibb Pharmaceutical Research Institute, PO Box 4000, Princeton, NJ 08543-4000, USA. lalgudi.harikrishnan@bms.com
Kamau
Muthoni G
MG
Herpin
Timothy F
TF
Morton
George C
GC
Liu
Yalei
Y
Cooper
Christopher B
CB
Salvati
Mark E
ME
Qiao
Jennifer X
JX
Wang
Tammy C
TC
Adam
Leonard P
LP
Taylor
David S
DS
Chen
Alice Ye A
AY
Yin
Xiaohong
X
Seethala
Ramakrishna
R
Peterson
Tara L
TL
Nirschl
David S
DS
Miller
Arthur V
AV
Weigelt
Carolyn A
CA
Appiah
Kingsley K
KK
O'Connell
Jonathan C
JC
Michael Lawrence
R
R
D001583:Benzoxazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D053480:Cholesterol Ester Transfer Proteins / Q000037:antagonists & inhibitors* / Q000378:metabolism; D006801:Humans; D008958:Models, Molecular; D015394:Molecular Structure; D013329:Structure-Activity Relationship
D001583:Benzoxazoles; D053480:Cholesterol Ester Transfer Proteins