Zobrazeno 1 - 10
of 23
pro vyhledávání: '"Sharon Tong"'
Autor:
Dong-Ming Shen, Michael Wolff, Shirly Pinto, Deodial Guiadeen, Bindhu V. Karanam, James M. Balkovec, Arto D. Krikorian, Shuwen He, Maria Madeira, Donald M. Sperbeck, Andreas Verras, Judyann Wiltsie, Jian Liu, Jackie Shang, Tim Cernak, Beth Ann Murphy, Qingmei Hong, Christine C. Chung, Ravi P. Nargund, Kevin D. Dykstra, Judith N. Gorski, Robert J. DeVita, Sharon Tong, Tianying Jian, Lisa M. Sonatore, Jeffrey T. Kuethe, Jianying Xiao, Jinqi Liu, Zhong Lai, Zhicai Wu, Mikhail Reibarkh, Ginger X. Yang, Yang Yu
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 29:1182-1186
Previously disclosed benzimidazole-based DGAT1 inhibitors containing a cyclohexane carboxylic acid moiety suffer from isomerization at the alpha position of the carboxylic acid group, generating active metabolites which exhibit DGAT1 inhibition compa
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6d804bc7e0890d2b1abe6ee34b194779
https://doi.org/10.1016/j.bmcl.2019.03.025
https://doi.org/10.1016/j.bmcl.2019.03.025
Autor:
Robert J. De Vita, Zhi-Cai Shi, Bindhu V. Karanam, Beth Ann Murphy, Shuwen He, Tianying Jian, Christine C. Chung, Maria Madeira, Qingmei Hong, Tim Cernak, Ravi P. Nargund, James M. Balkovec, Donald M. Sperbeck, Min Liu, Andreas Verras, Judyann Wiltsie, Jian Liu, Lisa M. Sonatore, Sharon Tong, Shirly Pinto, Deodial Guiadeen, Michael Wolff, Zhicai Wu, Dong-Ming Shen, Arto D. Krikorian, Yang Yu, Judith N. Gorski, Petr Vachal, Jianying Xiao, Jinqi Liu, Zhong Lai
Publikováno v:
Bioorganicmedicinal chemistry letters. 29(11)
The parallel medicinal chemistry (PMC) was effectively applied to accelerate the optimization of diacylglycerol O-acyltransferase I (DGAT-1) inhibitors. Through a highly collaborative and iterative library design, synthesis and testing, a benzimidazo
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5d0380ff27cfdf10ca6e079a9a149965
https://pubmed.ncbi.nlm.nih.gov/30952592
https://pubmed.ncbi.nlm.nih.gov/30952592
Autor:
Dann L. Parker, Randal M. Bugianesi, Birgit T. Priest, Feroze Ujjainwalla, Edward C. Sherer, Stanley Mitelman, Sharon Tong, Matthew Lombardo, William K. Hagmann, Ravi P. Nargund, Melissa Costa, Christopher Joseph Sinz, Anka G. Ehrhardt, Scott D. Edmondson, Ravi Kurukulasuriya, Xiaofang Li, Karen H. Dingley, Kate Bender, Kevin S. Ratliff, Jonathan E. Wilson
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 26:2947-2951
A novel series of benzo-[1,2,4]-triazolo-[1,4]-oxazepine GPR142 agonists are described. The series was designed to address the suboptimal PK (pharmacokinetic) and off-target profile of a class of N-aryl-benzo-[1,4]-oxazepine-4-carboxamides, represent
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::27f4fd9aaf407b2d77d08816feb7cb20
https://doi.org/10.1016/j.bmcl.2016.04.018
https://doi.org/10.1016/j.bmcl.2016.04.018
Autor:
Shirly Pinto, Deodial Guiadeen, David X. Yang, Tianying Jian, Ravi P. Nargund, Donald M. Sperbeck, Tim Cernak, Qingmei Hong, James M. Balkovec, Christine C. Chung, Dong-Ming Shen, Jeffrey T. Kuethe, Sharon Tong, Pauline C. Ting, Judyann Wiltsie, Jack Gibson, Lisa M. Sonatore, Zhicai Wu, Ginger X. Yang, Michael Wolff, Judith N. Gorski, Robert J. DeVita, Yang Yu, Jian Liu, JeanMarie Lisnock, Zhong Lai, Shuwen He, Jianying Xiao, Jinqi Liu, Bindhu V. Karanam, Arto D. Krikorian, Kevin D. Dykstra, Maria Madeira
Publikováno v:
ACS Medicinal Chemistry Letters. 5:1082-1087
We report the discovery of a novel series of DGAT1 inhibitors in the benzimidazole class with a piperdinyl-oxy-cyclohexanecarboxylic acid moiety. This novel series possesses significantly improved selectivity against the A2A receptor, no ACAT1 off-ta
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5736a4f35707b793d0b53f6a00a346de
https://doi.org/10.1021/ml5003426
https://doi.org/10.1021/ml5003426
Autor:
Donald Nelson, Gary G. Chicchi, James Dellureficio, Ravi P. Nargund, Peter H. Dobbelaar, Liangqin Guo, Kwei-Lan Tsao, Janet S. Kerr, Bei Zhang, Zhong Lai, Patricia R. Bunting, Shrenik K. Shah, Raman K. Bakshi, Qingmei Hong, Hongbo Qi, Guillermo Fernandez, Mikhail Reibarkh, Qing Shao, Quang Truong, Koppara Samuel, Jian Liu, Sylvia Volksdorf, Zhixiong Ye, Yun-Ping Zhou, Margaret Wu, Cai Li, Stan Mitelman, Andrew D. Howard, Wu Du, Maria E. Trujillo, George J. Eiermann, Shuwen He, Vijay Bhasker G. Reddy, Tianying Jian, Pierre Morissette, Patrick Fitzgerald, Dorina Trusca, Sharon Tong, William K. Hagmann
Publikováno v:
ACS Medicinal Chemistry Letters. 5:748-753
Antagonism of somatostatin subtype receptor 3 (sstr3) has emerged as a potential treatment of Type 2 diabetes. Unfortunately, the development of our first preclinical candidate, MK-4256, was discontinued due to a dose-dependent QTc (QT interval corre
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ced576c72131916fe1527dabb0d36e73
https://doi.org/10.1021/ml500028c
https://doi.org/10.1021/ml500028c
Autor:
David Won-Shik Kim, Ravi P. Nargund, Zhicai Wu, Maria Madeira, Jian Liu, JeanMarie Lisnock, Tianying Jian, Jeffrey T. Kuethe, Bindhu V. Karanam, Qingmei Hong, Dong-Ming Shen, Michael Wolff, Sharon Tong, Jack Gibson, Zhong Lai, Shirly Pinto, Deodial Guiadeen, Yang Yu, Donald M. Sperbeck, Beth Ann Murphy, James M. Balkovec, Christine C. Chung, Dunlu Chen, Judyann Wiltsie, Jinqi Liu, Xiaoli Chen, Shuwen He, Arto D. Krikorian, Lisa M. Sonatore, Pauline C. Ting, Judith N. Gorski, Robert J. DeVita, Ginger X. Yang
Publikováno v:
ACS Medicinal Chemistry Letters. 4:773-778
We report the design and synthesis of a series of novel DGAT1 inhibitors in the benzimidazole class with a pyridyl-oxy-cyclohexanecarboxylic acid moiety. In particular, compound 11A is a potent DGAT1 inhibitor with excellent selectivity against ACAT1
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::38cc6718ba0c1555d5839bf034018f4f
https://doi.org/10.1021/ml400168h
https://doi.org/10.1021/ml400168h
Autor:
D. Euan MacIntyre, Yue Feng, Lauren P. Shearman, Xiao-Ming Guan, Mark T. Goulet, Christopher W. Plummer, Sharon Tong, Quang Truong, D. Sloan Stribling, Donald J. Marsh, Junying Wang, Hong Yu, Kimberly Rosko, Sander G. Mills, Paul E. Finke, Alison M. Strack, Stephanie K. Spann, L. H. T. Van Der Ploeg, Shrenik K. Shah, Douglas J. MacNeil, Ramon E. Camacho, Joseph M. Metzger, William K. Hagmann, Tung M. Fong
Publikováno v:
European Journal of Pharmacology. 579:215-224
We document in vitro and in vivo effects of a novel, selective cannabinoid CB 1 receptor inverse agonist, Imidazole 24b (5-(4-chlorophenyl)- N -cyclohexyl-4-(2,4-dichlorophenyl)-1-methyl-imidazole-2-carboxamide). The in vitro binding affinity of Imid
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::49649d7b8bc67415f284cf71a0a449db
https://doi.org/10.1016/j.ejphar.2007.10.033
https://doi.org/10.1016/j.ejphar.2007.10.033
Autor:
Constantin Tamvakopolous, Rui Liang, Emma R. Parmee, Lauren Abrardo, Song Zheng, Bei B. Zhang, Sharon Tong, James R. Tata, Steve Mock, Michael Wright, Mari R. Candelore, Victor D.-H. Ding, Edward J. Brady, Richard Saperstein, Laurie Tota
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:587-592
A series of conformationally constrained tri-substituted ureas were synthesized, and their potential as glucagon receptor antagonists was evaluated. This effort resulted in the identification of compound 4a, which had a binding IC50 of 4.0 nM and was
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1fa30cbe651c82bd44e412b97a827a15
https://doi.org/10.1016/j.bmcl.2006.11.014
https://doi.org/10.1016/j.bmcl.2006.11.014
Autor:
Yang Yu, Gary G. Chicchi, Frederick Wong, Janet S. Kerr, Sharon Tong, Zhe Feng, Guillermo Fernandez, Edward C. Sherer, Kwei-Lan Tsao, Qing Shao, Bei B. Zhang, Yun-Ping Zhou, Pierre Morissette, Shuwen He, Shrenik K. Shah, Vijay Bhasker G. Reddy, Liangqin Guo, Ravi P. Nargund, Margaret Wu, Cai Li, Zhixiong Ye, Alexander Pasternak, George J. Eiermann, Patricia R. Bunting, Hongbo Qi, Michele Pachanski, Stan Mitelman, Maria E. Trujillo, Quang Truong, Maria Madiera, Andrew D. Howard, Donald Nelson, Qingmei Hong, Zhong Lai, Yue Feng, Bindhu V. Karanam, Jian Liu, Koppara Samuel, Wu Du, William K. Hagmann, Tianying Jian, Dorina Trusca, Sylvia Volksdorf, Peter H. Dobbelaar
Publikováno v:
ACS medicinal chemistry letters. 6(5)
The imidazolyl-tetrahydro-β-carboline class of sstr3 antagonists have demonstrated efficacy in a murine model of glucose excursion and may have potential as a treatment for type 2 diabetes. The first candidate in this class caused unacceptable QTc i
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8391d2d13678e95f2d50ddfa654d1520
https://pubmed.ncbi.nlm.nih.gov/26005524
https://pubmed.ncbi.nlm.nih.gov/26005524
Autor:
Rui Liang, Lauri M. Tota, Kevin T. Chapman, Joseph L. Duffy, Xiaodong Yang, Frank Xiaoqing Liu, Guoqiang Jiang, Edward J. Brady, Brian A. Kirk, Song Zheng, Zenon Konteatis, James R. Tata, Mari R. Candelore, Deborah Szalkowski, Sharon Tong, Bei B. Zhang, Victor D.-H. Ding, Elizabeth Louise Campbell, Richard Saperstein, Sajjad A. Qureshi, Dan Xie, Peter Zafian
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:1401-1405
A novel class of antagonists of the human glucagon receptor (hGCGR) has been discovered. Systematic modification of the lead compound identified substituents that were essential for activity and those that were amenable to further optimization. This
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::02875fe32941a428c96a4c4eb4d22e48
https://doi.org/10.1016/j.bmcl.2005.01.003
https://doi.org/10.1016/j.bmcl.2005.01.003