Zobrazeno 1 - 10
of 29
pro vyhledávání: '"Robert M, Rzasa"'
Autor:
Andrew Tasker, Andreas Reichelt, Yi-Ling Hu, Deanna Mohn, John McCarter, Ben Fisher, Robert M. Rzasa, Yi Chen, Julio C. Medina, Gang Yu, Sharon Wannberg, Brian Lucas, Ron C. Kelly, Jennifer Seganish, Felix Gonzalez-Lopez de Turiso, Xiaolin Hao, Kristin L. Andrews, Douglas A. Whittington, Matthew Frank Brown, Dawei Zhang, Youngsook Shin, Mario G. Cardozo, Jason Duquette, Robert C. Wahl, Leeanne Zalameda, Daniela Metz, Vatee Pattaropong, Michael G. Johnson, Tisha San Miguel, Randall W. Hungate, John Whoriskey, Lawrence R. McGee, Timothy D. Cushing, Kirk Henne, Liping H. Pettus, Xiao He
Publikováno v:
Journal of Medicinal Chemistry. 58:480-511
The development and optimization of a series of quinolinylpurines as potent and selective PI3Kδ kinase inhibitors with excellent physicochemical properties are described. This medicinal chemistry effort led to the identification of 1 (AMG319), a com
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::41f464b8458b3d559ce036ed30580e01
https://doi.org/10.1021/jm501624r
https://doi.org/10.1021/jm501624r
Autor:
Essa Hu, Samer Chmait, Thomas T. Nguyen, Amy Porter, Kristin L. Andrews, Silke Miller, Carl Davis, Jennifer R. Allen, Robert M. Rzasa, James J. S. Treanor, Alexander J. Pickrell, Adrie D. Jones, Roxanne Kunz, Daniel B. Horne, Xiaoning Zhao, Matthew R. Kaller, Holger Monenschein, Ning Chen, Heather Eastwood, Jeffrey Clarine, Michael J. Frohn, Andreas Reichelt
Publikováno v:
Bioorganic & Medicinal Chemistry. 22:6570-6585
We report the discovery of a novel series of 2-(3-alkoxy-1-azetidinyl) quinolines as potent and selective PDE10A inhibitors. Structure-activity studies improved the solubility (pH 7.4) and maintained high PDE10A activity compared to initial lead comp
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9a111fa0c0183c52c1f5301e3654201e
https://doi.org/10.1016/j.bmc.2014.10.013
https://doi.org/10.1016/j.bmc.2014.10.013
Autor:
Qingyian Liu, Kaustav Biswas, Frank Koegler, Tiffany L. Correll, Toni Williamson, Jodi Bradley, Jennifer R. Allen, Leeanne Zalameda, Darren L. Reid, Michael D. Bartberger, Joe Zhu, Stephen J. Wood, Randy Hungate, Yichin Liu, Frank Chavez, Robert M. Rzasa, Jianhua Zhang, John D. McCarter, Thomas Nixey, Paul H. Wen, Li Zhu, Shannon Rumfelt, Yi Luo, Safura Babu-Khan, Stephen Hitchcock, Ning Chen, Mqhele Ncube, Wenyuan Qian, Frenel Fils Demorin, Dean Hickman, Christopher M. Tegley, Jian J. Chen, Albert Amegadzie, Charles W. Dean, Chester Chenguang Yuan
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:6447-6454
γ-Secretase modulators (GSMs) are potentially disease-modifying treatments for Alzheimer's disease. They selectively lower pathogenic Aβ42 levels by shifting the enzyme cleavage sites without inhibiting γ-secretase activity, possibly avoiding know
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9f9717b5fcc1d773beec78fba83ce7ef
https://doi.org/10.1016/j.bmcl.2013.09.041
https://doi.org/10.1016/j.bmcl.2013.09.041
Autor:
Samer Chmait, Adrie D. Jones, Amy Porter, Kristin L. Andrews, Xiaoning Zhao, Jennifer R. Allen, Shannon Rumfelt, Wenge Zhong, Essa Hu, James R. Falsey, Robert M. Rzasa, Steven W. Louie, James J. S. Treanor, Ning Chen
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:7371-7375
We report the discovery of a novel series of biaryl ethers as potent and selective PDE10A inhibitors. Structure-activity studies improved the potency and decreased Pgp-mediated efflux found in the initial compound 4. X-ray crystallographic studies re
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6c902b8d3ff73465c5b07e532310cd1d
https://doi.org/10.1016/j.bmcl.2012.10.078
https://doi.org/10.1016/j.bmcl.2012.10.078
Autor:
David Powers, Guo-Qiang Cao, Scott Middleton, Lisa Sherman, Kelvin Sham, Dawei Zhang, Partha P. Chakrabarti, Faye Hsieh, Andrew Tasker, Yanyan Tudor, Bradley Henkle, Shimin Xu, Lu Min Wong, Ryan Wurz, Liping H. Pettus, Matthew R. Lee, Robert M. Rzasa, Violeta Yu, Christiaan J. M. Saris, Matthew H. Plant, Rashid Syed
Publikováno v:
Journal of Medicinal Chemistry. 51:6280-6292
The p38 mitogen-activated protein kinase (MAPK) is a central signaling molecule in many proinflammatory pathways, regulating the cellular response to a multitude of external stimuli including heat, ultraviolet radiation, osmotic shock, and a variety
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7087b9c4f5722d23b003b38ab86133ff
https://doi.org/10.1021/jm8005405
https://doi.org/10.1021/jm8005405
Autor:
Osslund Timothy D, Robert M. Rzasa, Ella Magal, Wenge Zhong, David Powers, Charles Henley, Jiandong Zhang, Weiya Wang, Thomas T. Nguyen, Hu Liu, Xiaoling Xiong, Matthew R. Kaller, Mark H. Norman, Hui-Ling Wang
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:5384-5389
Cyclin-dependent kinase 5 (CDK5) is a serine/threonine protein kinase and its deregulation is implicated in a number of neurodegenerative disorders such as Alzheimer's disease, amyotrophic lateral sclerosis, and ischemic stroke. Using active site hom
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::968546fb33db2e6af44d1045b89d8075
https://doi.org/10.1016/j.bmcl.2007.07.045
https://doi.org/10.1016/j.bmcl.2007.07.045
Autor:
Joseph M. Langenhan, Robert M. Rzasa, Kaapjoo Park, Daniel Romo, Luo Sun, and Alexander Akhiezer, Jun O. Liu, Helene A. Shea
Publikováno v:
Journal of the American Chemical Society. 120:12237-12254
The asymmetric synthesis of the potent immunosuppressive agent (−)-pateamine A isolated from the marine sponge Mycale sp. is described. A key strategy employed in the synthesis was a β-lactam-based macrocyclization to form the 19-membered dilacton
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::3b67d78ab55093e43dd2ccd14cadd796
https://doi.org/10.1021/ja981846u
https://doi.org/10.1021/ja981846u
Publikováno v:
ChemInform. 26
An asymmetric synthesis of the (E,Z)-hydroxydienoate2 and correlation to a pateamine A degradation product has enabled assignment of the absolute configuration of pateamine at C24 as (S).
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::6cbbfb4024aa029a235782aa94309e72
https://doi.org/10.1002/chin.199544268
https://doi.org/10.1002/chin.199544268
Publikováno v:
ChemInform. 29
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::589430e6bb4cb0f81eea34ad09a8adf4
https://doi.org/10.1002/chin.199824204
https://doi.org/10.1002/chin.199824204
Autor:
Robert M. Rzasa, Dawei Zhang, Oliver R. Thiel, Michal Achmatowicz, Robert D. Larsen, Andreas Reichelt, James R. Falsey
Publikováno v:
ChemInform. 41
An efficient and convenient method for the synthesis of [1,2,4]triazolo[4,3-a]pyridines was exemplified by the synthesis of 20 analogues bearing a variety of substituents at the 3-position. The methodology involves a palladium-catalyzed addition of h
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::238d11aa80eef9fc8ea6e1d1eac478a4
https://doi.org/10.1002/chin.201027148
https://doi.org/10.1002/chin.201027148