Zobrazeno 1 - 10
of 49
pro vyhledávání: '"Paul A Aristoff"'
Autor:
Karen G Anthony, Ulrich Strych, Kacheong R Yeung, Carolyn S Shoen, Oriana Perez, Kurt L Krause, Michael H Cynamon, Paul A Aristoff, Raymond A Koski
Publikováno v:
PLoS ONE, Vol 6, Iss 5, p e20374 (2011)
In an effort to discover new drugs to treat tuberculosis (TB) we chose alanine racemase as the target of our drug discovery efforts. In Mycobacterium tuberculosis, the causative agent of TB, alanine racemase plays an essential role in cell wall synth
Externí odkaz:
https://doaj.org/article/3e4a604a5b604dce8355e6a8c3ab559e
Autor:
Michel Ledizet, Karen Anthony, Michael H. Cynamon, Sara Mootien, Paul Kaplan, Michelle S. DeStefano, Kacheong R. Yeung, Oluwatoyin A. Asojo, Carolyn Shoen, Paul A. Aristoff, Raymond A. Koski, Pier F. Cirillo, Yashang Lee
Publikováno v:
Biochemical Pharmacology. 86:222-230
The genus Mycobacterium includes non-pathogenic species such as M. smegmatis, and pathogenic species such as M. tuberculosis, the causative agent of tuberculosis (TB). Treatment of TB requires a lengthy regimen of several antibiotics, whose effective
Autor:
Pier F. Cirillo, Thomas J. Powell, Michel Ledizet, Lin Leng, Oluwatoyin A. Asojo, Fengwei Bai, Mihai Ciustea, Raymond A. Koski, Karen Anthony, Richard Bucala, Paul A. Aristoff
Publikováno v:
Journal of Biological Chemistry. 287:30653-30663
Macrophage migration inhibitory factor (MIF) is a catalytic cytokine and an upstream mediator of the inflammatory pathway. MIF has broad regulatory properties, dysregulation of which has been implicated in the pathology of multiple immunological dise
Autor:
Michael H. Cynamon, Adriana E. Rosato, Michel Ledizet, Mihai Ciustea, Sara Mootien, Oriana A. Perez, Raymond A. Koski, Paul Kaplan, Karen Anthony, Pier F. Cirillo, Paul A. Aristoff, Kacheong R. Yeung
Publikováno v:
Biochemical Pharmacology. 83:368-377
Methicillin-resistant Staphylococcus aureus (MRSA) is a human pathogen and a major cause of hospital-acquired infections. New antibacterial agents that have not been compromised by bacterial resistance are needed to treat MRSA-related infections. We
Autor:
Betty H. Yagi, Judith C. Hamel, Judy K. Moerman, Ronda D. Schaadt, Gary E. Zurenko, Douglas Stapert, Paul Adrian Aristoff, Paul D. Johnson, Ford Charles W
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 13:4197-4200
Novel benzazepine oxazolidinone antibacterials were synthesized and evaluated against clinically relevant susceptible and resistant organisms. The effect of ring nitrogen position and N-substitution on antibacterial activity is examined.
Autor:
Lester A. Dolak, Johnson Paul D, Chong Kt, Harvey Irving Skulnick, Paul K. Tomich, Michael John Bohanon, Strohbach Joseph Walter, Suvit Thaisrivongs, Steve Turner, K. D. Watenpaugh, M.‐M. Horng, M.N. Janakiraman, R. R. Hinshaw, Paul A. Aristoff, J. C. Lynn, Eric P. Seest, Tommasi Ruben A
Publikováno v:
Journal of Medicinal Chemistry. 41:3467-3476
A broad screening program previously identified phenprocoumon (1) as a small molecule template for inhibition of HIV protease. Subsequent modification of this lead through iterative cycles of structure-based design led to the activity enhancements of
Autor:
Mariano Busso, Kuo-Chen Chou, W. Gary Tarpley, Kathleen M. Downey, Donna L. Romero, Paul A. Aristoff, Kellie M. Franks, Fritz Reusser, Richelle J. Lemay, Lionel Resnick, Ferenc J. Kezdy, Martin R. Deibel, Irene W. Althaus, Antero G. So, Richard C. Thomas
Publikováno v:
Biochemical Pharmacology. 51:743-750
U-31,355, or 4-amino-2-(benzylthio)-6-chloropyrimidine is an inhibitor of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase (RT) and possesses anti-HIV activity in HIV-1-infected lymphocytes grown in tissue culture. The compound acts
Autor:
J. C. Lynn, Tommasi Ruben A, Johnson Paul D, Strohbach Joseph Walter, R. R. Hinshaw, M.N. Janakiraman, Chong Kt, Turner, Paul A. Aristoff, Morge Rr, Howe Wj, Tomich Pk, Donna L. Romero, M.‐M. Horng, Barry C. Finzel, Carolyn Biles, K. D. Watenpaugh, Suvit Thaisrivongs
Publikováno v:
Journal of Medicinal Chemistry. 39:4630-4642
From a broad screening program, the 4-hydroxycoumarin phenprocoumon (I) was previously identified as a lead template with HIV protease inhibitory activity. The crystal structure of phenprocoumon/HIV protease complex initiated a structure-based design
Autor:
Suvit Thaisrivongs, Harvey I. Skulnick, Steve R. Turner, Joseph W. Strohbach, Ruben A. Tommasi, Paul D. Johnson, Paul A. Aristoff, Thomas M. Judge, Ronald B. Gammill, Jeanette K. Morris, Karen R. Romines, Robert A. Chrusciel, Roger R. Hinshaw, Kong-Teck Chong, W. Gary Tarpley, Susan M. Poppe, David E. Slade, Janet C. Lynn, Miao-Miao Horng, Paul K. Tomich, Eric P. Seest, Lester A. Dolak, W. Jeffrey Howe, Gina M. Howard, Francis J. Schwende, Lisa N. Toth, Guy E. Padbury, Grace J. Wilson, Lihua Shiou, Gail L. Zipp, Karen F. Wilkinson, Bob D. Rush, Mary J. Ruwart, Kenneth A. Koeplinger, Zhiyang Zhao, Serena Cole, Renee M. Zaya, Thomas J. Kakuk, Musiri N. Janakiraman, Keith D. Watenpaugh
Publikováno v:
Journal of Medicinal Chemistry. 39:4349-4353
Publikováno v:
Journal of Medicinal Chemistry. 36:1956-1963
A practical synthesis of CBI (2) was developed and applied to the synthesis of benzannelated analogs of CC-1065, including CBI-PDE-I-dimer (13) and CBI-bis-indole [(+)-A'BC]. The CBI-PDE-I-dimer was shown to have similar DNA sequence selectivity and