Zobrazeno 1 - 10
of 81
pro vyhledávání: '"Robert Zahler"'
Autor:
Yan Shi, Ying Wang, Wei Meng, Robert P. Brigance, Denis E. Ryono, Scott Bolton, Hao Zhang, Sean Chen, Rebecca Smirk, Shiwei Tao, Joseph A. Tino, Kristin N. Williams, Richard Sulsky, Laura Nielsen, Bruce Ellsworth, Michael K. Y. Wong, Jung-Hui Sun, Leslie W. Leith, Dawn Sun, Dauh-Rurng Wu, Anuradha Gupta, Richard Rampulla, Arvind Mathur, Bang-Chi Chen, Aiying Wang, Helen G. Fuentes-Catanio, Lori Kunselman, Michael Cap, Jacob Zalaznick, Xiaohui Ma, Heng Liu, Joseph R. Taylor, Rachel Zebo, Beverly Jones, Stephen Kalinowski, Joann Swartz, Ada Staal, Kevin O’Malley, Lisa Kopcho, Jodi K. Muckelbauer, Stanley R. Krystek, Steven A. Spronk, Jovita Marcinkeviciene, Gerry Everlof, Xue-Qing Chen, Carrie Xu, Yi-Xin Li, Robert A. Langish, Yanou Yang, Qi Wang, Kamelia Behnia, Aberra Fura, Evan B. Janovitz, Nicola Pannacciulli, Steven Griffen, Bradley A. Zinker, John Krupinski, Mark Kirby, Jean Whaley, Robert Zahler, Joel C. Barrish, Jeffrey A. Robl, Peter T. W. Cheng
Publikováno v:
Journal of Medicinal Chemistry. 65:4291-4317
Autor:
Ashraf Wilsily, Robert Zahler, Nan Ke, Claudio Chuaqui, Michael J. Bradley, Jason J. Marineau, Goran Malojčić, Stephane Ciblat, Anneli Savinainen, Darby Schmidt, Nigel J. Waters, Kristin B. Hamman, Sydney Alnemy, Stephanie Roy, Dana K. Winter, Anzhelika Kabro, Kenneth Matthew Whitmore, Shanhu Hu, Janessa Mihalich
Publikováno v:
Journal of medicinal chemistry. 65(2)
CDK7 has emerged as an exciting target in oncology due to its roles in two important processes that are misregulated in cancer cells: cell cycle and transcription. This report describes the discovery of SY-5609, a highly potent (sub-nM CDK7 Kd) and s
Autor:
Anthony Padfield, Patrick Barton, Laurence G. Rahme, Joanne Teague, Paul Turnpenny, Robert Zahler, Aileen Rubio, Michael J. Pucci
Publikováno v:
Journal of Pharmaceutical and Biomedical Analysis. 139:44-53
Alkyl quinolone molecules 2-heptyl-4-quinolone (HHQ) and 2-heptyl-3-hydroxy-4(1H)-quinolone (PQS) are important quorum sensing signals, which play a mediatory role in the pathogenesis of acute and chronic Pseudomonas aeruginosa infection. A targeted
Autor:
Michele Negri, Laurence G. Rahme, Sylvain Milot, Tomoe Kitao, Eric Déziel, Damien Maura, Melissa Starkey, Robert Zahler, Arunava Bandyopadhaya, François Lépine, Susanne Fetzner, Biliana Lesic, Mike Pucci, Steffen L. Drees, Antonio Felici
Publikováno v:
ACS Chemical Biology. 12:1435-1443
Pseudomonas aeruginosa is an important nosocomial pathogen that is frequently recalcitrant to available antibiotics, underlining the urgent need for alternative therapeutic options against this pathogen. Targeting virulence functions is a promising a
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
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
Autor:
Stanley R. Krystek, Donald Egan, John S. Sack, Joyce E. Kuhns, Alexandra A. Nirschl, Gary J. Grover, Rajasree Golla, John A. Lupisella, James A. Bryson, John D. Dimarco, Jack Z. Gougoutas, Ligaya M. Simpkins, Aberra Fura, Jacek Ostrowski, Yan Zou, Yi-Xin Li, Robert Zahler, Yongmi An, James C. Sutton, Kevin Kish, Viral Vyas, Lawrence G. Hamann, Ramakrishna Seethala, Paul G. Sleph, Blake C. Beehler
Publikováno v:
Journal of Medicinal Chemistry. 52:2794-2798
A novel selective androgen receptor modulator (SARM) scaffold was discovered as a byproduct obtained during synthesis of our earlier series of imidazolidin-2-ones. The resulting oxazolidin-2-imines are among the most potent SARMs known, with many ana
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
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
Autor:
David P. Rotella, Robert Zahler, David J. Augeri, Timur Gungor, Aiying Wang, William S. Slusarchyk, Scott A. Bolton, James C. Sutton, Jeffrey A. Robl, Zulan Pi, Karnail S. Atwal, Ligaya M. Simpkins, Yajun Liu, Chet Kwon, Lawrence G. Hamann, Rex A. Parker, Guohua Zhao, Mark S. Kirby, Zhong Sun, David R. Magnin, Jovita Marcinkeviciene, James G. Robertson
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:6476-6480
The synthesis and structure–activity relationships of novel dipeptidyl peptidase IV inhibitors replacing the classical cyanopyrrolidine P1 group with other small nitrogen heterocycles are described. A unique potency enhancement was achieved with β