Zobrazeno 1 - 10
of 115
pro vyhledávání: '"Ravi P. Nargund"'
Autor:
Chunhui Huang, Anandan Palani, Zhiqiang Yang, Qiaolin Deng, Vijay Reddy, Ravi P. Nargund, Songnian Lin, Simona Altezza, Elisabetta Bianchi, Federica Orvieto, Paul Carrington
Publikováno v:
ACS Medicinal Chemistry Letters. 13:1255-1261
The combination of insulin and incretin-based therapies has emerged as a potential promising tactic for the treatment of diabetes. Here we report the first example of a unimolecular triagonist to simultaneously target insulin, GLP-1, and glucagon rec
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::821409fc3f5b1f2b52d5869918f98800
https://doi.org/10.1021/acsmedchemlett.2c00218
https://doi.org/10.1021/acsmedchemlett.2c00218
Autor:
Dmitri A. Pissarnitski, Ahmet Kekec, Lin Yan, Yuping Zhu, Danqing D. Feng, Pei Huo, Christina Madsen-Duggan, Christopher R. Moyes, Ravi P. Nargund, Terri Kelly, Xiaoping Zhang, Ester Carballo-Jane, Judith Gorski, Peter Zafian, Mo Qatanani, Niels Kaarsholm, Fanyu Meng, Xiujuan Jia, Keun-Joong Lee, Weixun Wang, Sherrie Xu, Michael J. Hohn, Michael J. Iammarino, Mark A. McCoy, Grace A. Okoh, Yingkai Liang, Scott A. Hollingsworth, Mark D. Erion, David E. Kelley, Robert M. Garbaccio, Amy Zhang, James Mu, Songnian Lin
Publikováno v:
Journal of Medicinal Chemistry. 65:5593-5605
We have identified a series of novel insulin receptor partial agonists (IRPAs) with a potential to mitigate the risk of hypoglycemia associated with the use of insulin as an antidiabetic treatment. These molecules were designed as dimers of native in
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::159d29e98accab17d5d9616e44812b0d
https://doi.org/10.1021/acs.jmedchem.1c02073
https://doi.org/10.1021/acs.jmedchem.1c02073
Autor:
Barbara Pio, Ravi P. Nargund, Yan Guo, Daniel Kosinski, Josien Hubert B, Michael Wright, Michele Pachanski, Harry R. Chobanian, Xiaoping Zhang, Richard Tschirret-Guth, Melissa Kirkland, Andrew D. Howard, Sarah Souza, Eric R. Ashley, Robert K. Orr, Steven L. Colletti, Joel Mane, Jerry Di Salvo, Michael W. Miller, Boonlert Cheewatrakoolpong, Koppara Samuel, William K. Hagmann, James Lamca, Juliann Ehrhart, Maria E. Trujillo, Jackie Shang, Qing Chen, Adam B. Weinglass, Randal M. Bugianesi
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 29:1842-1848
GPR40 (FFAR1 or FFA1) is a G protein-coupled receptor, primarily expressed in pancreatic islet β-cells and intestinal enteroendocrine cells. When activated by fatty acids, GPR40 elicits increased insulin secretion from islet β-cells only in the pre
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::67130fd906c302e54806df711af08d1b
https://doi.org/10.1016/j.bmcl.2019.04.050
https://doi.org/10.1016/j.bmcl.2019.04.050
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:
Craig C. Correll, Robert G. Aslanian, Li Xiao, Rema Bitar, Wei Zhou, John W. Butcher, Charles G. Garlisi, Joshua Close, Rachel N. Maccoss, Joon Jung, Scott Crawford, Kevin M. Maloney, Purakkattle Biju, Anandan Palani, Xianhai Huang, Xiaoxin Yang, Kevin D. McCormick, Scott Peterson, Hongjun Zhang, Diane Rindgen, Ying Huang, Alexei V. Buevich, Ning Shao, Li Dong, Phieng Siliphaivanh, Jason D. Brubaker, Michelle Martinez, Hongchen Qiu, François G. Gervais, Ravi P. Nargund, Zhidan Liu
Publikováno v:
ACS Medicinal Chemistry Letters. 9:679-684
[Image: see text] A novel series of tricyclic tetrahydroquinolines were identified as potent and selective CRTh2 receptor antagonists. The agonism and antagonism switch was achieved through structure-based drug design (SBDD) using a CRTh2 receptor ho
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8efda955acd4eb892808b6d65e2545f5
https://doi.org/10.1021/acsmedchemlett.8b00145
https://doi.org/10.1021/acsmedchemlett.8b00145
Autor:
Ravi P. Nargund, Li-Kang Zhang, Xiaoxin Yang, Hongchen Qiu, Anandan Palani, Xianhai Huang, Craig C. Correll, Robert G. Aslanian, Wei Zhou, Ashwin U. Rao, Alexei V. Buevich, Charles G. Garlisi
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 27:5344-5348
New synthetic methods were developed for the preparation of 2,3,6-trisubstituted 1-oxo-1,2-dihydroisoquinolines as CRTh2 antagonists. The isoquinolinone core could be constructed before the introduction of substitution groups or synthesized through a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::b28d3bc2f1b1f9e4bbf4b1d0c1c38ddc
https://doi.org/10.1016/j.bmcl.2017.07.064
https://doi.org/10.1016/j.bmcl.2017.07.064
Autor:
Songnian Lin, Cannon B. Wille, Chunhui Huang, Vijay Bhasker G. Reddy, Huaibing He, Anandan Palani, Ravi P. Nargund
Publikováno v:
Tetrahedron Letters. 58:1219-1222
The late-stage modification of native peptides to alter and/or enhance their properties and functions is attractive but formidably challenging. Peptide lipidation is one of the effective strategies to overcome short half-life and rapid clearance. Her
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::aed3eea142f8d2dfc6f45ce31005a5d1
https://doi.org/10.1016/j.tetlet.2017.02.031
https://doi.org/10.1016/j.tetlet.2017.02.031
Autor:
Melissa Kirkland, Randal M. Bugianesi, Melodie Christensen, Maria E. Trujillo, Michele Pachanski, Richard Tschirret-Guth, Josien Hubert B, Adam B. Weinglass, Sarah Souza, Ravi P. Nargund, Christopher W. Plummer, Andrew D. Howard, Joel Mane, Louis-Charles Campeau, Robert K. Orr, Daniel Kosinski, Xiaoping Zhang, Boonlert Cheewatrakoolpong, Jerry Di Salvo, Michael W. Miller, William K. Hagmann, Helen Chen, Steven L. Colletti, Andrew Nolting, Michael Wright, Matthew J. Clements, Murali Rajagopalan
Publikováno v:
ACS Medicinal Chemistry Letters. 8:221-226
GPR40 is a G-protein-coupled receptor expressed primarily in pancreatic islets and intestinal L-cells that has been a target of significant recent therapeutic interest for type II diabetes. Activation of GPR40 by partial agonists elicits insulin secr
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6942c1dd589ae2364bd7ea069018de04
https://doi.org/10.1021/acsmedchemlett.6b00443
https://doi.org/10.1021/acsmedchemlett.6b00443
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