The class
Array synthesis optimizes a high-throughput screening hit into a novel 2-arylbenzoxazole CETP inhibitor series (Bioorg Med Chem Lett 2008)
Original title: 2-Arylbenzoxazoles as novel cholesteryl ester transfer protein inhibitors: optimization via array synthesis
A fluorescence-based high-throughput screen for CETP inhibitors identified 2-arylbenzoxazole 5 as an initial hit. Researchers then used array synthesis to systematically vary the A- and B-rings of the scaffold and investigate structure-activity relationships, establishing 2-arylbenzoxazoles as a novel chemical series for CETP inhibitor development and laying groundwork for the further benzoxazole optimization work that followed in subsequent years.
Original 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.
Summary written by cetpinhibition.org from the published abstract; figures as published. Page updated 19 August 2026. Methods.