| Literature DB >> 21094047 |
Florida Kallashi1, Dooseop Kim, Jennifer Kowalchick, You Jung Park, Julianne A Hunt, Amjad Ali, Cameron J Smith, Milton L Hammond, James V Pivnichny, Xinchun Tong, Suoyu S Xu, Matt S Anderson, Ying Chen, Suzanne S Eveland, Qiu Guo, Sheryl A Hyland, Denise P Milot, Anne-Marie Cumiskey, Melanie Latham, Laurence B Peterson, Raymond Rosa, Carl P Sparrow, Samuel D Wright, Peter J Sinclair.
Abstract
We describe structure-activity studies leading to the discovery of 2-arylbenzoxazole 3, the first in a series to raise serum high-density lipoprotein cholesterol levels in transgenic mice. Replacement of the 4-piperidinyloxy moiety with piperazinyl provided a more synthetically tractable lead, which upon optimization resulted in compound 4, an excellent inhibitor of cholesteryl ester transfer protein function with good pharmacokinetic properties and in vivo efficacy.Entities:
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Year: 2010 PMID： 21094047 DOI： 10.1016/j.bmcl.2010.10.062
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823