Zobrazeno 1 - 10
of 20
pro vyhledávání: '"Constance Farley"'
Autor:
Anandan Palani, Ashwin U. Rao, Xiao Chen, Xianhai Huang, Jing Su, Haiqun Tang, Ying Huang, Jun Qin, Dong Xiao, Sylvia Degrado, Michael Sofolarides, Xiaohong Zhu, Zhidan Liu, Brian McKittrick, Wei Zhou, Robert Aslanian, William J. Greenlee, Mary Senior, Boonlert Cheewatrakoolpong, Hongtao Zhang, Constance Farley, John Cook, Stan Kurowski, Qiu Li, Margaret van Heek, Gangfeng Wang, Yunsheng Hsieh, Fangbiao Li, Scott Greenfeder, Madhu Chintala
Publikováno v:
ACS Medicinal Chemistry Letters. 3:63-68
Structure-guided optimization of a series of C-5 alkyl substituents led to the discovery of a potent nicotinic acid receptor agonist SCH 900271 (33) with an EC50 of 2 nM in the hu-GPR109a assay. Compound 33 demonstrated good oral bioavailability in a
Autor:
William J. Greenlee, Jaroslava Paruchova, Blair Weig, Brian E. Hawes, John W. Clader, Daniel J. Weston, Mark D. McBriar, Kim O’Neill, Kathleen Cox, Constance Farley, Henry Guzik, Timothy J. Kowalski, Ruo Xu, Anandan Palani, Sherry Shapiro, Brian D. Spar, John Cook
Publikováno v:
Journal of Medicinal Chemistry. 49:2294-2310
Melanin-concentrating hormone (MCH) is a cyclic, nonadecapeptide expressed in the CNS of all vertebrates that regulates feeding behavior and energy homeostasis via interaction with the central melanocortin system. Regulation of this interaction resul
Autor:
Robert A. Del Vecchio, Brian E. Hawes, Steve Fried, Brian D. Spar, Blair Weig, Henry Guzik, Mark D. McBriar, Timothy J. Kowalski, Kim O’Neill, Constance Farley, Lorraine Ghibaudi, John W. Clader, Joyce J. Hwa, John Cook
Publikováno v:
European Journal of Pharmacology. 535:182-191
Melanin concentrating hormone (MCH) is a cyclic neuropeptide expressed in the lateral hypothalamus that plays an important role in energy homeostasis. To investigate the pharmacological consequences of inhibiting MCH signaling in murine obesity model
Publikováno v:
Obesity Research. 11:845-851
Objective: To characterize the meal patterns of free feeding Sprague-Dawley rats that become obese or resist obesity when chronically fed a high-fat diet. Research Methods and Procedures: Male Sprague-Dawley rats (N = 120) were weaned onto a high-fat
Autor:
Douglas S Compton, Harry R. Davis, Lizbeth M. Hoos, April Smith-Torhan, Margaret van Heek, Constance Farley
Publikováno v:
British Journal of Pharmacology. 138:1459-1464
Ezetimibe (1-(4-fluorophenyl)-(3R)-[3-(4-fluorophenyl)-(3S)-hydroxypropyl]-(4S)-(4-hydroxyphenyl)-2-azetidinone) and its analog SCH48461 are potent and selective cholesterol absorption inhibitors that inhibit the transport of cholesterol across the i
Publikováno v:
Obesity Research. 10:956-963
Objective: Childhood obesity is an emerging health problem. This study assesses the effects of three levels of dietary fat (10%, 32%, and 45% measured by kilocalories) on weight gain, body composition, energy metabolism, and comorbidity factors in ra
Publikováno v:
British Journal of Pharmacology. 134:409-417
1. Ezetimibe potently inhibits the transport of cholesterol across the intestinal wall, thereby reducing plasma cholesterol in preclinical animal models of hypercholesterolemia. The effect of ezetimibe on known absorptive processes was determined in
Autor:
Theodore M. Austin, Harry R. Davis, Glen Tetzloff, Constance Farley, Margaret van Heek, John Cook
Publikováno v:
Diabetes. 50:1330-1335
Ezetimibe potently and selectively inhibits cholesterol absorption in the intestine, thereby reducing plasma cholesterol in preclinical models of hypercholesterolemia. Clinical trials have demonstrated that ezetimibe lowers LDL cholesterol and raises
Autor:
Margaret van Heek, Lizbeth M. Hoos, Douglas S Compton, Kevin B. Alton, Harry R. Davis, Edmund J. Sybertz, Constance Farley
Publikováno v:
British Journal of Pharmacology. 129:1748-1754
Previous studies described the metabolism-based discovery of a potent, selective inhibitor of intestinal absorption of cholesterol, SCH58235 (Ezetimibe). Here we demonstrate that the phenolic glucuronide (SCH60663) of SCH58235, was more potent at inh
Autor:
Jean E. Lachowicz, Robert E. West, Joyce J. Hwa, Zhiwei Yang, Sie-Mun Lo, Gerald W. Shipps, Shuqin Zheng, Dinesh P. Sinha, Craig R. Mahon, Mark E. Cartwright, Yongqi Deng, Margaret van Heek, Alan S. Bass, Constance Farley
Publikováno v:
Bioorganicmedicinal chemistry letters. 23(3)
Inhibitors based on a benzo-fused spirocyclic oxazepine scaffold were discovered for stearoyl-coenzyme A (CoA) desaturase 1 (SCD1) and subsequently optimized to potent compounds with favorable pharmacokinetic profiles and in vivo efficacy in reducing