Zobrazeno 1 - 10
of 22
pro vyhledávání: '"Ravi Kurukulasuriya"'
Autor:
David A. Candito, Vladimir Simov, Anmol Gulati, Solomon Kattar, Ryan W. Chau, Blair T. Lapointe, Joey L. Methot, Duane E. DeMong, Thomas H. Graham, Ravi Kurukulasuriya, Mitchell H. Keylor, Ling Tong, Gregori J. Morriello, John J. Acton, Barbara Pio, Weiguo Liu, Jack D. Scott, Michael J. Ardolino, Theodore A. Martinot, Matthew L. Maddess, Xin Yan, Hakan Gunaydin, Rachel L. Palte, Spencer E. McMinn, Lisa Nogle, Hongshi Yu, Ellen C. Minnihan, Charles A. Lesburg, Ping Liu, Jing Su, Laxminarayan G. Hegde, Lily Y. Moy, Janice D. Woodhouse, Robert Faltus, Tina Xiong, Paul Ciaccio, Jennifer A. Piesvaux, Karin M. Otte, Matthew E. Kennedy, David Jonathan Bennett, Erin F. DiMauro, Matthew J. Fell, Santhosh Neelamkavil, Harold B. Wood, Peter H. Fuller, J. Michael Ellis
Publikováno v:
Journal of Medicinal Chemistry. 65:16801-16817
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::365ba0e1a6a6d085b4344b637344b726
https://doi.org/10.1021/acs.jmedchem.2c01605
https://doi.org/10.1021/acs.jmedchem.2c01605
Autor:
David A, Candito, Vladimir, Simov, Anmol, Gulati, Solomon, Kattar, Ryan W, Chau, Blair T, Lapointe, Joey L, Methot, Duane E, DeMong, Thomas H, Graham, Ravi, Kurukulasuriya, Mitchell H, Keylor, Ling, Tong, Gregori J, Morriello, John J, Acton, Barbara, Pio, Weiguo, Liu, Jack D, Scott, Michael J, Ardolino, Theodore A, Martinot, Matthew L, Maddess, Xin, Yan, Hakan, Gunaydin, Rachel L, Palte, Spencer E, McMinn, Lisa, Nogle, Hongshi, Yu, Ellen C, Minnihan, Charles A, Lesburg, Ping, Liu, Jing, Su, Laxminarayan G, Hegde, Lily Y, Moy, Janice D, Woodhouse, Robert, Faltus, Tina, Xiong, Paul, Ciaccio, Jennifer A, Piesvaux, Karin M, Otte, Matthew E, Kennedy, David Jonathan, Bennett, Erin F, DiMauro, Matthew J, Fell, Santhosh, Neelamkavil, Harold B, Wood, Peter H, Fuller, J Michael, Ellis
Publikováno v:
Journal of medicinal chemistry. 65(24)
Inhibition of leucine-rich repeat kinase 2 (LRRK2) kinase activity represents a genetically supported, chemically tractable, and potentially disease-modifying mechanism to treat Parkinson's disease. Herein, we describe the optimization of a novel ser
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::d1e71dbb505d333749f04ff7e2a07818
https://pubmed.ncbi.nlm.nih.gov/36475697
https://pubmed.ncbi.nlm.nih.gov/36475697
Autor:
Theodore A. Martinot, Xavier Fradera, Meredeth A. McGowan, Wensheng Yu, Heidi Ferguson, Purakattle J Biju, H. Zhou, Nicolas Solban, Qinglin Pu, Yongxin Han, Xiao Wang, Kun Liu, Ravi Kurukulasuriya, Yu-hong Lam, Abdelghani Achab, Karin M. Otte, Michael J. Ardolino, Amy C. Doty, Charles A. Lesburg, J. Richard Miller, Yongqi Deng, Mangeng Cheng, Hongjun Zhang, Ian Knemeyer, Nunzio Sciammetta, David Jonathan Bennett
Publikováno v:
ACS Med Chem Lett
[Image: see text] Checkpoint inhibitors have demonstrated unprecedented efficacy and are evolving to become standard of care for certain types of cancers. However, low overall response rates often hamper the broad utility and potential of these break
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c30fa3b8f261ace5c7d56e064b7047fa
https://doi.org/10.1021/acsmedchemlett.9b00344
https://doi.org/10.1021/acsmedchemlett.9b00344
Optimization of brain-penetrant picolinamide derived leucine-rich repeat kinase 2 (LRRK2) inhibitors
Autor:
Blair T. Lapointe, Jack D. Scott, Xin Cindy Yan, Haiqun Tang, Janice D Woodhouse, Kaleen Konrad Childers, Robert Faltus, Erin F. DiMauro, Solomon Kattar, Charles S. Yeung, Ravi Kurukulasuriya, Vladimir Simov, Hakan Gunaydin, Anmol Gulati, Joey L. Methot, Rachel L. Palte, Ellen C. Minnihan, Greg Morriello, J. Michael Ellis, Harold B. Wood, Santhosh Neelamkavil, Karin M. Otte, Michael J. Ardolino, Barbara Pio, Ping Liu, Laxminarayan G Hegde, Matthew J. Fell, Vanessa L. Rada, Peter Fuller, Paul J Ciaccio
Publikováno v:
RSC Med Chem
The discovery of potent, kinome selective, brain penetrant LRRK2 inhibitors is the focus of extensive research seeking new, disease-modifying treatments for Parkinson's disease (PD). Herein, we describe the discovery and evolution of a picolinamide-d
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6c8d45ea7dd7adda70471298a4476afa
https://europepmc.org/articles/PMC8292993/
https://europepmc.org/articles/PMC8292993/
Autor:
Jinchu Liu, Maarten Hoek, Qiang Tan, Andreas Verras, Don Gauthier, Tim Cernak, Kevin D. Dykstra, Anthony Ogawa, Yun-Fang Yang, Shane W. Krska, Robert J. DeVita, Dong-Ming Shen, Beata Zamlynny, Thomas Bateman, Ravi Kurukulasuriya, Yili Chen, Lisa DiMichelle, Kun Liu, Alejandro Crespo, Petr Vachal, Jeffrey Madwed, Kendall N. Houk
Publikováno v:
Bioorganicmedicinal chemistry letters. 29(14)
The derivatization of pharmaceuticals is a core activity in the discovery and development of new medicines. Late-stage functionalization via modern C H functionalization chemistry has emerged as a powerful technique with which to diversify advanced p
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9397cb2536275f111ddd3b473f58897d
https://pubmed.ncbi.nlm.nih.gov/31104995
https://pubmed.ncbi.nlm.nih.gov/31104995
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:
Vincent J. Colandrea, Ravi Kurukulasuriya, Petr Vachal, Beth Ann Murphy, Rajan Anand, Kake Zhao, Mikhail Reibarkh, Alejandro Crespo, Ruth A. Duffy, Joseph L. Duffy, Jonathan E. Wilson, Anne-Marie Cumiskey, Maud Reiter, Aaron Zwicker, Fengqi Zhang, Kaushik Mitra, Douglas G. Johns
Using the collective body of known (CETP) inhibitors as inspiration for design, a structurally novel series of tetrahydroquinoxaline CETP inhibitors were discovered. An exemplar from this series, compound 5, displayed potent in vitro CETP inhibition
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::50f1f63cab482d2b7431e81a19537bcf
https://europepmc.org/articles/PMC4789658/
https://europepmc.org/articles/PMC4789658/
Publikováno v:
Current Topics in Medicinal Chemistry. 7:569-578
Xanthines and xanthine-like DPP-IV inhibitors were first disclosed in 2002. Since then, several dozen accounts of xanthine-based DPP-IV inhibitors have been published. Only a few presentations and journal articles have appeared, with the vast majorit
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d84b7e2697bf57a4dbab07a5755ba861
https://doi.org/10.2174/156802607780091073
https://doi.org/10.2174/156802607780091073
Autor:
Jiahong Wang, DeAnne Stolarik, Hovis M. Imade, Victoria Knourek-Segel, Phong Nguyen, Denise Wilcox, Peer B. Jacobson, Michael E. Brune, William Chiou, Steven Fung, Robin Shapiro, Vince Yeh, J.T. Link, Ravi Kurukulasuriya, Katina Monzon, Eugene N. Bush
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:5555-5560
A series of metabolically stable butyrolactam 11beta-HSD1 inhibitors have been synthesized and biologically evaluated. These compounds exhibit excellent HSD1 potency and HSD2 selectivity, pharmacokinetic, and pharmacodynamic profiles.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::16d60418fa06ac90a6a4054cde3829be
https://doi.org/10.1016/j.bmcl.2006.08.034
https://doi.org/10.1016/j.bmcl.2006.08.034
Autor:
William J. Chiou, Jiahong Wang, Jyoti R. Patel, Peer B. Jacobson, Michael E. Brune, J.T. Link, Ravi Kurukulasuriya, Hong Yong, Hing L. Sham, Steven Fung, Katina Monzon, DeAnne Stolarik, Hovis M. Imade, David W A Beno, Vince Yeh
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:5414-5419
A series of metabolically stable adamantane amide 11beta-HSD1 inhibitors have been synthesized and biologically evaluated. These compounds exhibit excellent HSD1 potency and HSD2 selectivity and good pharmacokinetic and pharmacodynamic profiles.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::401f7c072da604f9bdd8ef80c7fb5c64
https://doi.org/10.1016/j.bmcl.2006.07.055
https://doi.org/10.1016/j.bmcl.2006.07.055