Zobrazeno 1 - 10
of 26
pro vyhledávání: '"Jonathan N. Bauman"'
Autor:
Jonathan N. Bauman, Angela C. Doran, Amanda King-Ahmad, Raman Sharma, Gregory S. Walker, Jian Lin, Tsung H. Lin, Jean-Baptiste Telliez, Sakambari Tripathy, Theunis C. Goosen, Christopher Banfield, Bimal K. Malhotra, Martin E. Dowty
Publikováno v:
Drug Metabolism and Disposition. 50:1106-1118
Abrocitinib is an oral once-daily Janus kinase 1 selective inhibitor being developed for the treatment of moderate-to-severe atopic dermatitis. This study examined the disposition of abrocitinib in male participants following oral and intravenous adm
Autor:
Kentaro Futatsugi, Mary Ellen Banker, David W. Piotrowski, Kun Song, Michael Herr, Jonathan N. Bauman, Steven B Co, Sophie Y. Lavergne, Stephen W. Wright, Paula M. Loria, Liuqing Wei, Agustin Casimiro-Garcia, Wenhua Jiao, Matthew F. Sammons, Donna N. Petersen
Publikováno v:
Journal of Medicinal Chemistry. 61:1086-1097
A novel series of morpholine-based nonsteroidal mineralocorticoid receptor antagonists is reported. Starting from a pyrrolidine HTS hit 9 that possessed modest potency but excellect selectivity versus related nuclear hormone receptors, a series of li
Autor:
Linda S. Wood, Jonathan N. Bauman, Jian Lin, Bimal Malhotra, Martin E. Dowty, Xin Yang, Pankaj Gupta, Christopher Banfield, Theunis C. Goosen, Angela C. Doran, Jillian G. Johnson
Publikováno v:
Drug Metabolism and Pharmacokinetics. 35:S80
Autor:
Heather Eng, Jonathan N. Bauman, Robert L. Dow, M. G. Finn, Theunis C. Goosen, S.R. Chirapu, Timothy J. Strelevitz, Subhash C. Sinha
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 24:1144-1147
A design for the selective release of drug molecules in the liver was tested, involving the attachment of a representative active agent by an ester linkage to various 2-substituted 5-aminovaleric acid carbamates. The anticipated pathway of carboxyles
Autor:
Steven Hansel, Jonathan N. Bauman, Amit S. Kalgutkar, Thomas S. McDonald, Yue Chen, Raman Sharma, Angela Wolford, Heather Eng
Publikováno v:
Drug Metabolism and Disposition. 40:1067-1075
The United States Public Health Service Administration is alerting medical professionals that a substantial percentage of cocaine imported into the United States is adulterated with levamisole, a veterinary pharmaceutical that can cause blood cell di
Autor:
Spiros Liras, Cayla M. McEwen, Rushia A. Turner, David Price, Taha Rezai, Amit S. Kalgutkar, Roger G. Linington, Alan M. Mathiowetz, R. Scott Lokey, Matthew P. Jacobson, Arthur C Rand, Yizhong Zhang, Vladimir Gelev, Chad M. Renzelman, Siegfried S. F. Leung, Tina R White, Jonathan N. Bauman
Publikováno v:
Nature chemical biology
Backbone N-methylation is common among peptide natural products and has a substantial impact on both the physical properties and the conformational states of cyclic peptides. However, the specific impact of N-methylation on passive membrane diffusion
Autor:
John R. Soglia, Hao Sun, Jonathan N. Bauman, Zhuang Miao, Jianke Li, Angel Guzman-Perez, Kenneth J. DiRico, Tim F. Ryder, Scott W. Bagley, Kosea S. Frederick, Bruce M. Bechle, Sabrina X. Zhao, Michael P. Zawistoski, Daniel P. Walker, Kevin K.-C. Liu, Mary Theresa Didiuk, Amit S. Kalgutkar, Joel Morris, Robert M. Oliver, Ryan Michael Kelley, John William Benbow, David A. Griffith, Chandra Prakash
Publikováno v:
Chemical Research in Toxicology. 23:1115-1126
The synthesis and structure-activity relationship studies on 5-trifluoromethylpyrido[4,3-d]pyrimidin-4(3H)-ones as antagonists of the human calcium receptor (CaSR) have been recently disclosed [ Didiuk et al. ( 2009 ) Bioorg. Med. Chem. Lett. 19 , 45
Autor:
Gayatri Balan, Paul S. Humphries, David Price, Liuqing Wei, David W. Piotrowski, Holly A. Simmons, James A. Southers, Yan Zhang, Mayda Castrodad, Vishwas M. Paralkar, Amit S. Kalgutkar, Jonathan N. Bauman, Y. Li, Constantin Neagu, Hong Qi, Mei Li, Sandra M. Jennings, Robert M. Oliver, Samit Kumar Bhattacharya, Michael Herr, Kimberly Lazarra, David R. Healy, Vishal Khot, Brendon Kapinos
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:3328-3332
The design and profile of a series of zwitterionic calcium sensing receptor negative allosteric modulators is described. Evaluation of key analogues using a rat model demonstrate a robust response, significantly improved potency over ronacaleret and
Autor:
Jiri Aubrecht, Janvi Paralkar, Jonathan N. Bauman, Kim F. McClure, Santo R. Cortina, Amit S. Kalgutkar
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:1559-1563
The biochemical basis for S9-dependent mutagenic response of the 5-HT(2C) receptor agonist and diazinylpiperazine derivative 1 in the Salmonella Ames assay involves P450-mediated bioactivation to DNA-reactive quinone-methide, aldehyde and nitrone int
Autor:
David D. Boyer, Daniel P. Walker, Karki Kapil Kumar, Amit S. Kalgutkar, Brendon Kapinos, Jonathan N. Bauman
Publikováno v:
Drug Metabolism and Disposition. 37:999-1008
Prediction of the metabolic sites for new compounds, synthesized or virtual, is important in the rational design of compounds with increased resistance to metabolism. The aim of the present investigation was to use rational design together with MetaS