Zobrazeno 1 - 10
of 18
pro vyhledávání: '"Joel R Hardink"'
Autor:
Manisha Shah, Dexing Huang, Tony Blick, Andrea Connor, Lawrence A Reiter, Joel R Hardink, Conor C Lynch, Mark Waltham, Erik W Thompson
Publikováno v:
PLoS ONE, Vol 7, Iss 1, p e29615 (2012)
We investigated the effects of the matrix metalloproteinase 13 (MMP13)-selective inhibitor, 5-(4-{4-[4-(4-fluorophenyl)-1,3-oxazol-2-yl]phenoxy}phenoxy)-5-(2-methoxyethyl) pyrimidine-2,4,6(1H,3H,5H)-trione (Cmpd-1), on the primary tumor growth and br
Externí odkaz:
https://doaj.org/article/403a71d5b97340b1adaf0dad03567717
Autor:
John Schafer, Michael A. Plotkin, Xiaoyuan Ding, Todd Wisialowski, Meghan Maloney, Judith C. Hamel, Sandra P. McCurdy, Joel R. Hardink, Christopher Zook, Steven M. Finegan, Chakrapani Subramanyam, Lori Brennan, Rose Barham, Steven J. Brickner, Daniel P. Uccello, Dale Gordon Mcleod, Kwansik Yoon, Michael D. Huband, Jeffrey M. Casavant, Usa Reilly, Mark J. Mitton-Fry, Anthony Marfat, Richard P. Zaniewski, Gregory G. Stone, Thuy Hoang
Publikováno v:
Bioorganicmedicinal chemistry letters. 27(15)
Novel (non-fluoroquinolone) inhibitors of bacterial type II topoisomerases (NBTIs) are an emerging class of antibacterial agents. We report an optimized series of cyclobutylaryl-substituted NBTIs. Compound 14 demonstrated excellent activity both in v
Autor:
Rose Barham, Thuy Hoang, Jeremy T. Starr, Jennifer A. Young, M. Megan Lemmon, Joseph Penzien, Mark J. Mitton-Fry, Thomas M. Harris, Antonia A. Nikitenko, Brian S. Gerstenberger, Sandra P. McCurdy, Veerabahu Shanmugasundaram, Lisa Mullins, Joel R. Hardink, Jeffrey M. Casavant, Eric S. Marr, Jian Lin, Seungil Han, Joel T. Arcari, John P. Mueller, Brandon P. Schuff, Mark S. Plummer, Craig J. McPherson, Michael D. Huband, Mark C. Noe, Manjinder S. Lall, Richard P. Zaniewski, Chao Li, Matthew Frank Brown, Jianmin Sun, Eric B. McElroy, Andrew P. Tomaras
Publikováno v:
Journal of Medicinal Chemistry. 56:5541-5552
Herein we describe the structure-aided design and synthesis of a series of pyridone-conjugated monobactam analogues with in vitro antibacterial activity against clinically relevant Gram-negative species including Pseudomonas aeruginosa , Klebsiella p
Autor:
Magee Thomas Victor, Thuy-Trinh Nguyen, Joseph A. Abramite, Yue Shen, Jian Lin, Jiri Aubrecht, Fadia Dib-Hajj, Jeremy T. Starr, Alita A. Miller, Matthew Frank Brown, Shawn H. MacVane, Michael D. Huband, Li Zhang, Karl Granskog, Bryan Li, Jinshan Michael Chen, James M. McKim, John P. O'Donnell, Karen L. Leach, Paul C. Wilga, David P. Nicolau, Sandra P. McCurdy, Mark Edward Flanagan, Antonia F. Stepan, Andrew P. Tomaras, Mark C. Noe, Michael Kuhn, Scott B. Seibel, Rebecca Irvine, Jinfeng Xu, David C. Ackley, David R. Luke, Jared L. Crandon, Joel R. Hardink, Andrew Butler
Publikováno v:
Journal of Medicinal Chemistry. 56:5079-5093
We report novel polymyxin analogues with improved antibacterial in vitro potency against polymyxin resistant recent clinical isolates of Acinetobacter baumannii and Pseudomonas aeruginosa . In addition, a human renal cell in vitro assay (hRPTEC) was
Autor:
Hongying Gao, Jennifer A. Young, Joel R. Hardink, Veerabahu Shanmugasundaram, Steven M. Finegan, David Pattavina, Joel T. Arcari, Jian Lin, Jianmin Sun, Mark J. Mitton-Fry, Thuy Hoang, Matthew Frank Brown, Hud Lawrence Risley, Rebecca Irvine, Mark Edward Flanagan, Brandon P. Schuff, Seungil Han, Manjinder S. Lall, Brian S. Gerstenberger, Mark Niosi, Thomas M. Harris, Michael D. Huband, Chao Li, Lisa Mullins, Sandra P. McCurdy, M. Megan Lemmon, John P. Mueller, Jennifer Winton, Jeffrey M. Casavant, Mark S. Plummer, Mark C. Noe, Joseph Penzien, Jeremy T. Starr, David M. George
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:5989-5994
Novel siderophore-linked monobactams with in vitro and in vivo anti-microbial activity against MDR Gram-negative pathogens are described.
Autor:
Francis J. Sweeney, Thomas J. Carty, Marcie Vaughn, John A. Barberia, Joel M. Hawkins, Christopher Tokar, Lori L. Lopresti-Morrow, Mark C. Noe, Jennifer L. Liras, V. Natarajan, Sue A. Yocum, Sheri L. Snow, Peter G. Mitchell, Joel R. Hardink, Lisa M. Reeves
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:2808-2811
A series of pipecolic hydroxamate inhibitors of MMP-13 and aggrecanase was discovered based on screening known inhibitors of TNF-alpha converting enzyme (TACE). Potency versus aggrecanase was optimized by modification of the benzyloxyarylsulfonamide
Autor:
Joel R. Hardink, Michael A. Letavic, Chul Yu, Mark C. Noe, Francis J. Sweeney, Ethan J. Stam, Marcie Vaughn, Lisa M. Reeves, John T. Barberia, Jennifer L. Liras, Sheri L. Snow, Peter G. Mitchell, Thomas J. Carty, Lori L. Lopresti-Morrow
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 13:3243-3246
A series of novel MMP-13 and TNF-α converting enzyme inhibitors based on piperazine 2-hydroxamic acid scaffolds are described. The TACE, MMP-1 and MMP-13 activity of these inhibitors as well as the effect of substitution of the piperazine nitrogen a
Autor:
James P. Driscoll, Kwansik Yoon, Sandra P. McCurdy, Joel R. Hardink, Xiaoyuan Ding, Wei Yuan, Erbing Hua, Christopher Zook, Michael A. Plotkin, James F. Smith, Tao Chen, Steven J. Brickner, Meghan Maloney, Lori Brennan, Dale Gordon Mcleod, Anthony Marfat, Jeffrey M. Casavant, Richard M. Shepard, John Schafer, Usa Reilly, Shaughn Robinson, Judith C. Hamel, Chakrapani Subramanyam, Mark J. Mitton-Fry, Michael D. Huband, Michael Chen, Gregory G. Stone, Thuy Hoang, Richard P. Zaniewski
Publikováno v:
Bioorganicmedicinal chemistry letters. 23(10)
A structurally novel set of inhibitors of bacterial type II topoisomerases with potent in vitro and in vivo antibacterial activity was developed. Dual-targeting ability, hERG inhibition, and pharmacokinetic properties were also assessed.
Autor:
Andrea Connor, Erik W. Thompson, Mark Waltham, Tony Blick, Conor C. Lynch, Joel R. Hardink, Manisha H Shah, Lawrence A. Reiter, Dexing Huang
Publikováno v:
PLoS ONE, Vol 7, Iss 1, p e29615 (2012)
PLoS ONE
PLoS ONE
We investigated the effects of the matrix metalloproteinase 13 (MMP13)-selective inhibitor, 5-(4-{4-[4-(4-fluorophenyl)-1,3-oxazol-2-yl]phenoxy}phenoxy)-5-(2-methoxyethyl) pyrimidine-2,4,6(1H,3H,5H)-trione (Cmpd-1), on the primary tumor growth and br
Autor:
Jeffrey Van Deusen, Richa Chandra, Mamadou Wele, Abdoulaye Djimde, Connor O'Brien, Joel R. Hardink, Marcus R. Pereira, Jian Lin, David A. Fidock, Amar Bir Singh Sidhu, Philipp P. Henrich, David J. Johnson, Katrina Gore
Publikováno v:
Antimicrobial agents and chemotherapy. 55(7)
Evidence of emerging Plasmodium falciparum resistance to artemisinin-based combination therapies, documented in western Cambodia, underscores the continuing need to identify new antimalarial combinations. Given recent reports of the resurgence of chl