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Autor:
Xiaohong Zhu, Piwinski John J, Robbie L. McLeod, Tony Priestley, Shirley M. Williams, Robert G. Aslanian, Steve Sorota, Xiao-Yi Du, Xue-Song Zhang, Robert E. West, John A. Hey
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:5043-5047
In the late 1980's reports linking the non-sedating antihistamines terfenadine and astemizole with torsades de pointes, a form of ventricular tachyarrhythmia that can degenerate into ventricular fibrillation and sudden death, appeared in the clinical
Autor:
Robert Huryk, Piwinski John J, Cynthia Seidel-Dugan, Alexei V. Buevich, Ning Shao, Anandan Palani, Xianhai Huang, Robert G. Aslanian
Publikováno v:
Synthesis. 2009:2855-2872
A novel PhI(OAc) 2 -mediated oxidative cyclization reaction is discovered for the synthesis of α-oxy N-acyl aminals and hemiaminals in good yields from readily synthesized N-acyl enamines. This methodology represents a cascade process to construct t
Publikováno v:
Journal of Mass Spectrometry. 44:203-213
In vitro drug metabolism study is an integral part of drug discovery process. In this report, we have described the application of LTQ-Orbitrap hybrid mass spectrometer in conjunction with online hydrogen (H)/deuterium (D) exchange high resolution (H
Autor:
Xiao Tong, Sony Agrawal, Latha G. Nair, Melissa Blackman, Francisco Velazquez, Girijavallabhan, John Pichardo, Andrea Hart, Robert Chase, Srikanth Venkatraman, Kevin X. Chen, N.-Y. Shih, F. G. Njoroge, Stephane L. Bogen, Andrew Prongay, K.-C. Cheng, Piwinski John J, Wen-Lian Wu
Publikováno v:
Journal of Medicinal Chemistry. 52:336-346
Hepatitis C virus (HCV) infection is the major cause of chronic liver disease, leading to cirrhosis and hepatocellular carcinoma, and affects more than 200 million people worldwide. Although combination therapy of interferon-alpha and ribavirin is re
Autor:
Piwinski John J, Neng-Yang Shih, Robert E. West, Shirley M. Williams, Robert G. Aslanian, Vaccaro Henry A, Xiaohong Zhu
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:5032-5036
A series of non-imidazole histamine H(3) receptor antagonists based on the (3-phenoxypropyl)amine motif, which is a common pharmacophore for H(3) antagonists, has been identified. A preliminary SAR study around the amine moiety has identified 8a as a
Publikováno v:
Organic Letters. 10:2517-2520
A mild catalytic system to access diversely functionalized benzylic sulfonamides has been developed. Palladium-catalyzed alpha-arylation by Negishi cross-coupling of sulfonamide-stabilized anions and a wide range of aryl iodides, bromides, and trifla
Publikováno v:
Accounts of Chemical Research. 41:50-59
More than 170 million people worldwide are affected by the hepatitis C virus (HCV). The disease has been described as a "silent epidemic" and "a serious global health crisis". HCV infection is a leading cause of chronic liver disease such as cirrhosi
Autor:
Piwinski John J, Chander S. Celly, Rongze Kuang, Ping Wu, Pauline C. Ting, Ling Lin, Li Xiao, David J. Blythin, John H. Schwerdt, Xiang Zhang, Ho-Jane Shue, M. Motasim Billah, Xiaohong Zhu, Michael Minnicozzi, Ji Zhang, Neng-Yang Shih, Daniel Prelusky, Peng Wang, Robert G. Aslanian, Danlin Gu, Xiao Chen
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:5150-5154
Substituted quinolyl oxazoles were discovered as a novel and highly potent series of phosphodiesterase 4 (PDE4) inhibitors. Structure-activity relationship studies revealed that the oxazole core, with 4-carboxamide and 5-aminomethyl groups, is a nove
Autor:
Weidong Pan, Prudence Bradley, Kevin X. Chen, Parekh Tejal N, Andrea Hart, Frank Bennett, Danial Prelusky, Srikanth Venkatraman, Robert Chase, Susan Bogdanowich-Knipp, Jianshe Kong, Bancha Vibulbhan, Viyyoor M. Girijavallabhan, Hendrata Siska, Rong Kong, Weiying Yang, Kuo-Chi Cheng, Ashit K. Ganguly, Nancy Butkiewicz, Ashok Arasappan, Yuhua Huang, Andrew Prongay, Bruce A. Malcolm, Xiang Liang, Rong Liu, Xiaoming Cui, Walter A. Korfmacher, Sony Agrawal, Wanli Wu, Zhuyan Guo, Stephane L. Bogen, Pike Russell E, Ronald E. White, Jesse Wong, Yi-Tsung Liu, Jean-Marc Brisson, John Pichardo, Anil K. Saksena, Pavlovsky Anastasia, Bahige M. Baroudy, F. George Njoroge, Vincent Madison, Patrick Pinto, Santhanam Bama, Raymond G. Lovey, Edwin Jao, Lisa Broske, Veljko Popov, Yunsheng Hsieh, Paul Ingravallo, Sumei Ruan, Piwinski John J
Publikováno v:
Journal of Medicinal Chemistry. 49:6074-6086
Hepatitis C virus (HCV) infection is the major cause of chronic liver disease, leading to cirrhosis and hepatocellular carcinoma, which affects more than 170 million people worldwide. Currently the only therapeutic regimens are subcutaneous interfero