Zobrazeno 1 - 10
of 18
pro vyhledávání: '"Denise P. Milot"'
Autor:
Xinchun Tong, Melanie Latham, Ying Chen, Denise P. Milot, Milton L. Hammond, Amjad Ali, Eugene Tan, Sheryl A. Hyland, Carl P. Sparrow, Qiu Guo, Joann B. Napolitano, Laurence B. Peterson, Samuel D. Wright, Suoyu S. Xu, Qiaolin Deng, Yi-Heng Chen, Gayle E. Taylor, Zhijian Lu, Peter J. Sinclair, Suzanne S. Eveland, Matt S. Anderson
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:199-203
SAR studies of the substitution effect on the central phenyl ring of the biphenyl scaffold were carried out using anacetrapib (9a) as the benchmark. The results revealed that the new analogs with substitutions to replace trifluoromethyl (9a) had a si
Autor:
Milton L. Hammond, Anne-Marie Cumiskey, Sheryl A. Hyland, Ray Rosa, Christopher F. Thompson, Amjad Ali, Ying Chen, Suoyu S. Xu, James V. Pivnichny, Xinchun Tong, Qiu Guo, Hong Li, Carl P. Sparrow, Peter J. Sinclair, Joann B. Napolitano, Melanie Latham, Zhijian Lu, Samuel D. Wright, Laurence B. Peterson, Matt S. Anderson, Suzanne S. Eveland, Cameron J. Smith, Gayle E. Taylor, Denise P. Milot
Publikováno v:
Journal of Medicinal Chemistry. 54:4880-4895
The development of the structure-activity studies leading to the discovery of anacetrapib is described. These studies focused on varying the substitution of the oxazolidinone ring of the 5-aryloxazolidinone system. Specifically, it was found that sub
Autor:
Carl P. Sparrow, Milton L. Hammond, Denise P. Milot, Peter J. Sinclair, Suzanne S. Eveland, Ramzi F. Sweis, Ying Chen, Samuel D. Wright, Florida Kallashi, Julianne A. Hunt, Qiu Guo, Melanie Latham, Sheryl A. Hyland, Anne-Marie Cumiskey, Ray Rosa, Matt S. Anderson, Larry Peterson
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:1890-1895
The development of 2-phenylbenzoxazoles as inhibitors of cholesteryl ester transfer protein (CETP) is described. Initial efforts aimed at engineering replacements for the aniline substructures in the benchmark molecule. Reversing the connectivity of
Autor:
Dooseop Kim, Qiu Guo, Ying Chen, Milton L. Hammond, Xinchun Tong, Carl P. Sparrow, Amjad Ali, Denise P. Milot, Sheryl A. Hyland, Peter J. Sinclair, Samuel D. Wright, James V. Pivnichny, Julianne A. Hunt, Suoyu S. Xu, Cameron J. Smith, Florida Kallashi, Suzanne S. Eveland, You Jung Park, Matt S. Anderson, Melanie Latham, Ray Rosa, Jennifer E. Kowalchick, Anne-Marie Cumiskey, Laurence B. Peterson
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:558-561
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 p
Autor:
Suzanne S. Eveland, Laurence B. Peterson, Carl P. Sparrow, Zhijian Lu, Denise P. Milot, Amjad Ali, Joann B. Napolitano, Qiu Guo, Sheryl A. Hyland, Eugene Tan, Suoyu S. Xu, Samuel D. Wright, Ying Chen, Milton L. Hammond, Melanie Latham, Peter J. Sinclair, Ashleigh B. Theberge, Matt S. Anderson, Xinchun Tong
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:7469-7472
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.
Autor:
Ying Chen, Ken S. Koblan, Nadine Elowe, Mollie Ranalletta, Brian K. Hubbard, Timothy S. Fisher, Carl P. Sparrow, Ayesha Sitlani, Denise P. Milot, Mike Kavana, Elaine Tung, Gene Porter, Margarita Garcia-Calvo, Kathleen K. Bierilo, Peter J. Sinclair, Qing Chen, George H. Addona, Edward A. O'Neill, Suzanne S. Eveland, Caroline Houde, Betsy Frantz-Wattley
Publikováno v:
Journal of Lipid Research, Vol 51, Iss 9, Pp 2739-2752 (2010)
Cholesteryl ester transfer protein (CETP) has been identified as a novel target for increasing HDL cholesterol levels. In this report, we describe the biochemical characterization of anacetrapib, a potent inhibitor of CETP. To better understand the m
Autor:
Matt S. Anderson, Denise P. Milot, Xinchun Tong, Ying Chen, Suzanne S. Eveland, Florida Kallashi, James V. Pivnichny, Silvia Gonzalez, Carl P. Sparrow, Julianne A. Hunt, Samuel D. Wright, Sheryl A. Hyland, Suoyu S. Xu, Qiu Guo, Milton L. Hammond, Peter J. Sinclair
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:1019-1022
The development of a series of 2-arylbenzoxazole alpha-alkoxyamide and beta-alkoxyamine inhibitors of cholesteryl ester transfer protein (CETP) is described. Highly fluorinated alpha-alkoxyamides proved to be potent inhibitors of CETP in vitro, and t
Autor:
Suzanne S. Eveland, Paul Zuck, Sheryl A. Hyland, Wesley Tanaka, Marc Ferrer, Berta Strulovici, Omar F Laterza, Ying Chen, Matt S. Anderson, Qiu Guo, John A. Wagner, Samuel D. Wright, Laurence B. Peterson, Gregory O'Donnell, Carl P. Sparrow, Denise P. Milot, Sylvie Jezequel-Sur, Deborah Hilliard
Publikováno v:
Analytical Biochemistry. 368:239-249
Cholesteryl ester transfer protein (CETP) is a serum component responsible for both cholesteryl ester and triglyceride trafficking between high-density lipoprotein (HDL) and the apolipoprotein B (apoB)-containing very low-density lipoprotein (VLDL) a
Autor:
Denise P. Milot, Jacqueline C. Lopez, Laurence B. Peterson, Alan D. Adams, Samuel D. Wright, Jayne Chin, Lyndon J. Mitnaul, Sandra E. Rex-Rabe, Erik G. Lund, Carl P. Sparrow, John G. Menke, Jenny Tian, My-Hanh Lam, Melanie Latham, Ray Rosa, Shaei Huang, Qiu Guo, Charlotte Burton
Publikováno v:
Biochemical Pharmacology. 71:453-463
Liver X receptor (LXR) alpha and LXRbeta are closely related nuclear receptors that respond to elevated levels of intracellular cholesterol by enhancing transcription of genes that control cholesterol efflux and fatty acid biosynthesis. The consequen
Autor:
Joel P. Berger, Melba Hernandez, Wei Han, Carl P. Sparrow, Chhabi Biswas, Joanne Baffic, James V. Heck, Pei-Ran Wang, Samuel D. Wright, Gaochao Zhou, Yu-Sheng Chao, Qiu Guo, David E. Moller, Karen L. MacNaul, Denise P. Milot, Ranjit C. Desai, Neelam Sharma, Soumya P. Sahoo, Marc C. Ippolito, My-Hanh Lam, Linda J. Kelly, Margaret Wu, Thomas W. Doebber
Publikováno v:
Endocrinology. 145:1640-1648
Patients with type 2 diabetes mellitus exhibit hyperglycemia and dyslipidemia as well as a markedly increased incidence of atherosclerotic cardiovascular disease. Here we report the characterization of a novel arylthiazolidinedione capable of lowerin