2-Arylbenzoxazoles as novel cholesteryl ester transfer protein inhibitors: optimization via array synthesis

Lalgudi S Harikrishnan; Muthoni G Kamau; Timothy F Herpin; George C Morton; Yalei Liu; Christopher B Cooper; Mark E Salvati; Jennifer X Qiao; Tammy C Wang; Leonard P Adam; David S Taylor; Alice Ye A Chen; Xiaohong Yin; Ramakrishna Seethala; Tara L Peterson; David S Nirschl; Arthur V Miller; Carolyn A Weigelt; Kingsley K Appiah; Jonathan C O'Connell; R Michael Lawrence

doi:10.1016/j.bmcl.2008.03.030

2-Arylbenzoxazoles as novel cholesteryl ester transfer protein inhibitors: optimization via array synthesis

Bioorg Med Chem Lett. 2008 Apr 15;18(8):2640-4. doi: 10.1016/j.bmcl.2008.03.030. Epub 2008 Mar 14.

Affiliation

¹ Bristol-Myers Squibb Pharmaceutical Research Institute, PO Box 4000, Princeton, NJ 08543-4000, USA. lalgudi.harikrishnan@bms.com

PMID: 18374566
DOI: 10.1016/j.bmcl.2008.03.030

Abstract

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.

MeSH terms

Benzoxazoles / chemical synthesis*
Benzoxazoles / chemistry
Benzoxazoles / pharmacology*
Cholesterol Ester Transfer Proteins / antagonists & inhibitors*
Cholesterol Ester Transfer Proteins / metabolism
Humans
Models, Molecular
Molecular Structure
Structure-Activity Relationship

Substances

Benzoxazoles
Cholesterol Ester Transfer Proteins