Zobrazeno 1 - 10
of 50
pro vyhledávání: '"Thomas W. Doebber"'
Autor:
Peter T. Meinke, Weiguo Liu, Thomas W. Doebber, Joel P. Berger, Margaret E. McCann, Kun Liu, Taro E. Akiyama, Ching H. Chang, Harold B. Wood, Monica Einstein
Publikováno v:
Journal of Medicinal Chemistry. 52:4443-4453
A series of 3-acylindole-1-benzylcarboxylic acids were designed and synthesized while searching for a PPARgamma modulator with additional moderate intrinsic PPARalpha agonistic activity. 2-[3-[[3-(4-Chlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-ind
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::802686640bba3450cc48eb32ea072ccb
https://doi.org/10.1021/jm900367w
https://doi.org/10.1021/jm900367w
Autor:
Zhihua Li, Joel P. Berger, Raynald Bergeron, Alan D. Adams, Thomas W. Doebber, Jun Yao, John Woods, Bei B. Zhang, Emanuel Zycband, David E. Moller, Cherrie Liu
Publikováno v:
Endocrinology. 147:4252-4262
Peroxisome proliferator-activated receptor (PPAR)-gamma agonists are insulin sensitizers, whereas PPAR alpha agonists are lipid-lowering agents in humans. Chronic treatment with PPAR gamma agonists has been shown to prevent the onset of diabetes in y
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5d2e93a614f8708b10c6106567b5a1c1
https://doi.org/10.1210/en.2005-1535
https://doi.org/10.1210/en.2005-1535
Autor:
Arun K. Agrawal, Thomas W. Doebber, Pei-Ran Wang, Daniel J. Miller, James V. Heck, Julia K. Boueres, Marc C. Ippolito, Soumya P. Sahoo, Linda J. Kelly, Samuel D. Wright, Yu-Sheng Chao, Hiroo Koyama, A. Brian Jones, Gaochao Zhou, Joel P. Berger, David E. Moller, Ronald B. Franklin, Karen L. MacNaul, Ranjit C. Desai, Margaret Wu
Publikováno v:
Journal of Medicinal Chemistry. 47:3255-3263
A series of chromane-2-carboxylic acid derivatives was synthesized and evaluated for PPAR agonist activities. A structure-activity relationship was developed toward PPARalpha/gamma dual agonism. As a result, (2R)-7-(3-[2-chloro-4-(4-fluorophenoxy)phe
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b2f8f7be20ef0493afda0cab77841421
https://doi.org/10.1021/jm030621d
https://doi.org/10.1021/jm030621d
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::175dcc68b6952d7d3f93601399fd22f8
https://doi.org/10.1210/en.2003-1270
https://doi.org/10.1210/en.2003-1270
Autor:
Michael J. Forrest, Zao Hu, Roger Meurer, Alan D. Adams, Alex Elbrecht, Thomas W. Doebber, Joel P. Berger, Derek Von Langen, Adonis Dadiz, A. Brian Jones, David E. Moller, Karen L. MacNaul, Gaochao Zhou
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 13:3185-3190
A new class of O-arylmandelic acid PPAR agonists show excellent anti-hyperglycemic efficacy in a db/db mouse model of DM2. These PPARα-weighted agonists do not show the typical PPARγ associated side effects of BAT proliferation and cardiac hypertro
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::f27d9bf40d7785a422d3d9005c964c77
https://doi.org/10.1016/s0960-894x(03)00702-9
https://doi.org/10.1016/s0960-894x(03)00702-9
Autor:
Dominick F. Gratale, James V. Heck, David E. Moller, Karen L. MacNaul, Hiroo Koyama, Edward Metzger, Soumya P. Sahoo, Victoria K. Lombardo, Ronald B. Franklin, Thomas W. Doebber, Wei Han, Joel P. Berger, Ranjit C. Desai, Kwan Leung
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 13:3541-3544
A series of novel aryloxazolidine-2,4-diones was synthesized. A structure–activity relationship study of these compounds led to the identification of potent, orally active PPAR dual α/γ agonists. Based on the results of efficacy studies in the db
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f648cc526319a858cb2f0fdb3f282753
https://doi.org/10.1016/s0960-894x(03)00785-6
https://doi.org/10.1016/s0960-894x(03)00785-6
Autor:
John Ventre, Mona Parikh, Thomas W. Doebber, Bruce A. Johnson, Ann Petro, Gaochao Zhou, Joel Berger, Bei B. Zhang, Linda J. Kelly, Neelam Sharma, Michael R. Tanen, Alan D. Adams, Chhabi Biswas, Ralph T. Mosley, Richard S. Surwit, Alex Elbrecht, G. Marie Thompson, David E. Moller, Karen L. MacNaul, Karen Richards
Publikováno v:
Molecular Endocrinology. 17:662-676
Antidiabetic thiazolidinediones (TZDs) and non-TZD compounds have been shown to serve as agonists of the peroxisome proliferator-activated receptor gamma (PPARgamma). Here, we report the identification and characterization of a novel non-TZD selectiv
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fc313c36fc3c5d00f1f4f35a62207650
https://doi.org/10.1210/me.2002-0217
https://doi.org/10.1210/me.2002-0217
Autor:
Soumya P. Sahoo, Conrad Santini, Richard L. Tolman, Wei Han, Gregory D. Berger, Margaret Wu, Joel P. Berger, Ralph T. Mosley, Thomas W. Doebber, David E. Moller, Karen L. MacNaul
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 13:1277-1280
Beginning with the weakly active lead structure 1, a new series of hPPAR agonists was developed. In vivo glucose and triglyceride lowering activity was obtained by homologation and oxamination to 3, then conversion to substituted benzisoxazoles 4 and
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::65f5cca2eb75c9517c59ac716b777a7f
https://doi.org/10.1016/s0960-894x(03)00115-x
https://doi.org/10.1016/s0960-894x(03)00115-x
Autor:
Conrad Santini, Zao Hu, Alan D. Adams, Winston Yuen, Joel P. Berger, A. Brian Jones, David E. Moller, Karen L. MacNaul, Thomas W. Doebber
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 13:931-935
A series of amphipathic 3-phenylbenzisoxazoles were found to be potent agonists of human PPARalpha, gamma and delta. The optimization of acid proximal structure for in vitro and in vivo potency is described. Results of po dosed efficacy studies in th
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f01acf1ac7c27fa6b9b5716801c0eba9
https://doi.org/10.1016/s0960-894x(02)01029-6
https://doi.org/10.1016/s0960-894x(02)01029-6
Autor:
David E. Moller, Qing Dallas-Yang, Thomas W. Doebber, Gaochao Zhou, Xiaolan Shen, Deborah Szalkowski, Franklin Liu, Zhihua Li, Margaret Wu, Guoqiang Jiang, Bei B. Zhang, Joel Berger
Publikováno v:
Diabetes. 51:2412-2419
Thiazolidinediones (TZDs), agonists of peroxisome proliferator-activated receptor-gamma (PPARgamma), improve insulin sensitivity in vivo, and the mechanism remains largely unknown. In this study, we showed that, in Zucker obese (fa/fa) rats, acute (1
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bc90d7c56473d20471e868a2802f547b
https://doi.org/10.2337/diabetes.51.8.2412
https://doi.org/10.2337/diabetes.51.8.2412