Zobrazeno 1 - 10
of 31
pro vyhledávání: '"Thomas Harrity"'
Autor:
Ji Jiang, James Neels, David A. Gordon, Ruth R. Wexler, Alice Ye A. Chen, Michael Basso, Jon J. Hangeland, Leonard P. Adam, Heather Finlay, Paul G. Sleph, Lynn M. Abell, Richard Yang, Thomas Harrity, R. Michael Lawrence, David S. Taylor, Lauren Haque, Christine Huang, Xiaohong Yin, Todd J. Friends, Joelle M. Onorato
Publikováno v:
ACS Medicinal Chemistry Letters. 9:673-678
[Image: see text] Screening of a small set of nonselective lipase inhibitors against endothelial lipase (EL) identified a potent and reversible inhibitor, N-(3-(3,4-dichlorophenyl)propyl)-3-hydroxy-1-methyl-2-oxo-1,2-dihydropyridine-4-carboxamide (5;
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f785fa1a2ceebdbf57f8010e5dea4a83
https://doi.org/10.1021/acsmedchemlett.8b00138
https://doi.org/10.1021/acsmedchemlett.8b00138
Autor:
Paul E. Morin, Haixia Wang, Lawrence J. Kennedy, Stephen P. O'connor, James J. Li, Akbar Nayeem, Vidhyashankar Ramamurthy, Steven Sheriff, Nathan Morgan, Steven J. Walker, Xiang-Yang Ye, Frederick Moulin, Brad D. Maxwell, Thomas Harrity, Jeffrey A. Robl, Stephanie Y. Chen, Timothy W. Harper, Rachel Zebo, Jun Li, Zhenqiu Hong, Shung Wu, Mengmeng Wang, Randolph P. Ponticiello, David A. Gordon, Rajasree Golla, Ramakrishna Seethala, Daniel M. Camac, Joseph R. Taylor, David S. Yoon
[Image: see text] BMS-823778 (2), a 1,2,4-triazolopyridinyl-methanol derived analog, was identified as a potent and selective inhibitor of human 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD-1) enzyme (IC(50) = 2.3 nM) with >10,000-fold selectiv
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::537bf023154f9aff48423a9bc7df61b2
https://europepmc.org/articles/PMC6295842/
https://europepmc.org/articles/PMC6295842/
Autor:
Carrie Xu, George C. Morton, Vinayak Hosagrahara, Shung Wu, Denis E. Ryono, Jonathan Lippy, Narayanan Hariharan, Kenneth T. Locke, Xiang-Xang Ye, Wei Wang, Liqun Gu, Yi-Xin Li, Fucheng Qu, Peter T. W. Cheng, Sean S. Chen, Kevin O’Malley, Michael Cap, Robert Zahler, Tao Wang, Lori Kunselman, Charles Z. Ding, Cuixia Chu, Rebecca A. Smirk, Neil Flynn, Pratik Devasthale, Hao Zhang, Nathan Morgan, Atsu Apedo, Thomas Harrity, Lisa Zhang, Dennis Farrelly, Arthur M. Doweyko, Zhi Lai, Tim Herpin, Pathanjali Kadiyala
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 25:1196-1205
The design, synthesis and structure–activity relationships of a novel series of 3,4-disubstituted pyrrolidine acid analogs as PPAR ligands is outlined. In both the 1,3- and 1,4-oxybenzyl pyrrolidine acid series, the preferred stereochemistry was sh
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ef9c9221e9206ed0e57f44f10281d7ab
https://doi.org/10.1016/j.bmcl.2015.01.066
https://doi.org/10.1016/j.bmcl.2015.01.066
Autor:
Steven J. Walker, Vidyhashankar Ramamurthy, Jun Li, Shung Wu, David K. Leahy, John D. Dimarco, Brad D. Maxwell, Daniel M. Camac, Joseph R. Taylor, Akbar Nayeem, Zhiwei Guo, James J. Li, Xiang-Yang Ye, Frederick Moulin, Paul E. Morin, Stepen P O’Connor, Haixia Wang, Jeffrey A. Robl, Rachel Zebo, Mark S. Kirby, Thomas Harrity, Joel C. Barrish, Timothy W. Harper, Lawrence L Kennedy, Rajasree Golla, Atsu Apedo, Bogdan Sleczka, Yi-Xin Li, David S. Yoon, Bin He, Steven Sheriff, Ramakrishna Seethala, Nathan Morgan, Mengmeng Wang, Randolph P. Ponticiello, Raymond P. Scaringe, Stephanie Y. Chen, Jianqing Li, Zhenqiu Hong, Ronald L. Hanson, David A. Gordon
Publikováno v:
Journal of medicinal chemistry. 60(12)
BMS-816336 (6n-2), a hydroxy-substituted adamantyl acetamide, has been identified as a novel, potent inhibitor against human 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) enzyme (IC50 3.0 nM) with >10000-fold selectivity over human 11β-hydrox
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d86602b708c78e42f5648acb482b306b
https://pubmed.ncbi.nlm.nih.gov/28537398
https://pubmed.ncbi.nlm.nih.gov/28537398
Autor:
Ramakrishna Seethala, Steven J. Walker, Jun Li, Stephen P. O'connor, Lawrence J. Kennedy, Steven Sheriff, Rachel Zebo, Daniel M. Camac, Paul E. Morin, Jeffrey A. Robl, Joseph R. Taylor, James J. Li, Haixia Wang, Thomas Harrity, David A. Gordon, Akbar Nayeem, Timothy W. Harper, Zhenqiu Hong, Mengmeng Wang, Randolph P. Ponticiello, Rajasree Golla, Nathan Morgan
Publikováno v:
ACS Medicinal Chemistry Letters. 5:803-808
Small alkyl groups and spirocyclic-aromatic rings directly attached to the left side and right side of the 1,2,4-triazolopyridines (TZP), respectively, were found to be potent and selective inhibitors of human 11β-hydroxysteroid dehydrogenase-type 1
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9f50571624276edc8a5db39e2719422c
https://doi.org/10.1021/ml500144h
https://doi.org/10.1021/ml500144h
Autor:
Yaqun Zhang, Dianlin Xie, Kevin Kish, Aiying Wang, Stephen P. O'connor, Wei Meng, Herbert E. Klei, Huji Turdi, Lawrence G. Hamann, Robert Zahler, Jovita Marcinkeviciene, Robert Paul Brigance, Thomas Harrity, James K. Tamura, Aberra Fura, Carolyn A. Weigelt, Chao Hannguang J, Mark S. Kirby
Publikováno v:
Journal of Medicinal Chemistry. 53:5620-5628
Continued structure-activity relationship (SAR) exploration within our previously disclosed azolopyrimidine containing dipeptidyl peptidase-4 (DPP4) inhibitors led us to focus on an imidazolopyrimidine series in particular. Further study revealed tha
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::53ca7c24a1f6700c83b6ed4ef874c797
https://doi.org/10.1021/jm100634a
https://doi.org/10.1021/jm100634a
Autor:
Doree F. Sitkoff, Ming Chang, Carolyn A Cuff, Bang-Chi Chen, Cort S. Madsen, Xiaohong Yin, Saleem Ahmad, Evan B. Janovitz, Richard A. Reeves, Thomas Harrity, Lawrence J. Kennedy, Carol S. Ryan, Hossain Monshizadegan, Van Nguyen-Tran, Tong Li, Robert Zahler, Michael A. Blanar, Khehyong Ngu, Philip D. Stein, Rongan Zhang, Sharon N. Bisaha, Christine Huang, Joel C. Barrish, Eileen Bird, Debra Search, Celia D’Arienzo, Mary Giancarli, Robert Setters, Rulin Zhao, Jeffrey A. Robl, Xing Chen, Shaobin Zhuang
Publikováno v:
Journal of Medicinal Chemistry. 51:2722-2733
3-hydroxy-3-methylglutaryl coenzyme-A reductase (HMGR) inhibitors, more commonly known as statins, represent the gold standard in treating hypercholesterolemia. Although statins are regarded as generally safe, they are known to cause myopathy and, in
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b90d3adf6a8d7ca839916f3bce8ae5a0
https://doi.org/10.1021/jm800001n
https://doi.org/10.1021/jm800001n
Autor:
Lori Kunselman, Narayanan Hariharan, Pathanjali Kadiyala, Kenneth T. Locke, Denis E. Ryono, Thomas Harrity, Wei Wang, Arthur M. Doweyko, Randy Ponticiello, Liqun Gu, Pratik Devasthale, Lisa Zhang, Dennis Farrelly, Rachel Zebo, Michael Cap, Robert Zahler, Jodi K. Muckelbauer, Chiehying Chang, Cuixia Chu, Peter T. W. Cheng, Kevin O’Malley, Nathan Morgan, Litao Zhang, Jonathan Lippy, Vinayak Hosagrahara
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:1939-1944
A novel class of azetidinone acid-derived dual PPARalpha/gamma agonists has been synthesized for the treatment of diabetes and dyslipidemia. The preferred stereochemistry in this series for binding and functional agonist activity against both PPARalp
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c8bfbf6fa4536695047baca135da5c60
https://doi.org/10.1016/j.bmcl.2008.01.126
https://doi.org/10.1016/j.bmcl.2008.01.126
Autor:
Bang-Chi Chen, Neil Flynn, R. Michael Lawrence, Rulin Zhao, Ching-Hsuen Chu, James J. Li, Vito G. Sasseville, Scott A. Biller, Luping Chen, Randy Ponticiello, Haixia Wang, Dora M. Schnur, Dong Cheng, Jamil Haris, Jeffrey A. Robl, Kristen Pike, Joseph A. Tino, Mary T. Obermeier, Thomas Harrity, Timothy F. Herpin, Ramesh Padmanabha
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:3208-3211
A novel series of 2-hydroxy-N-arylbenzenesulfonamides were identified to be ATP-citrate lyase (ACL) inhibitors with compound 9 displaying potent in vitro activity (IC(50)=0.13 microM). Chronic oral dosing of compound 9 in high-fat fed mice lowered pl
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::863f1596275d02b6a6a0c62e58561a4d
https://doi.org/10.1016/j.bmcl.2007.03.017
https://doi.org/10.1016/j.bmcl.2007.03.017
Autor:
Narayanan Hariharan, Kasim A. Mookhtiar, Liqun Gu, Jimmy Ren, Chen Sean, Ramakrishna Seethala, Michael Cap, Lori Kunselman, Min Zhou, Peter T. W. Cheng, William Fenderson, Chunning Shao, Cuixia Chu, Scott A. Biller, Hao Zhang, Fucheng Qu, Pratik Devasthale, Dennis Farrelly, Jeon Yoon T, Randolph P. Ponticiello, John R. Wetterau, Wei Wang, Wen-Pin Yang, Thomas Harrity, Aaron Tieman, Denis E. Ryono, Richard E. Gregg
Publikováno v:
Diabetes. 55:240-248
Muraglitazar, a novel dual (alpha/gamma) peroxisome proliferator-activated receptor (PPAR) activator, was investigated for its antidiabetic properties and its effects on metabolic abnormalities in genetically obese diabetic db/db mice. In db/db mice
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::e4d94ba455d51e1e5f39b4a1484a6b08
https://doi.org/10.2337/diabetes.55.01.06.db05-0648
https://doi.org/10.2337/diabetes.55.01.06.db05-0648