Zobrazeno 1 - 10
of 45
pro vyhledávání: '"Philip D. Stein"'
Autor:
Maria L. Webb, Ilana L. Stroke, Laurie J. Sturzenbecker, David W. Hilbert, Brett A. Marinelli, Joan E. Sabalski, Linh Ma, David J. Diller, Philip D. Stein, Jeffrey J. Letourneau, Jorge Quintero
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 28:756-761
The discovery, synthesis and preliminary structure-activity relationship (SAR) of a novel class of inhibitors of Clostridium difficile (C. difficile) toxin B (TcdB) is described. A high throughput screening (HTS) campaign resulted in the identificati
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f742445d139a1bd6814035c6c49dc34f
https://doi.org/10.1016/j.bmcl.2018.01.005
https://doi.org/10.1016/j.bmcl.2018.01.005
Autor:
Yanfang Li, Jeffrey J. Letourneau, Laurie J. Sturzenbecker, Maria L. Webb, Brett A. Marinelli, Philip D. Stein, Ilana L. Stroke, Linh Ma, Andrew G. Cole, Igor Pechik, Jorge Quintero, David W. Hilbert, Joan E. Sabalski
Publikováno v:
Bioorganicmedicinal chemistry letters. 28(23-24)
Synthesis and structure-activity relationships (SAR) of a novel series of benzodiazepinedione-based inhibitors of Clostridium difficile toxin B (TcdB) are described. Compounds demonstrating low nanomolar affinity for TcdB, and which possess improved
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::090c6be502149e94cd4e282caaf0f29c
https://pubmed.ncbi.nlm.nih.gov/30392779
https://pubmed.ncbi.nlm.nih.gov/30392779
Autor:
Joan E. Sabalski, Yan Xu, Philip D. Stein, Laurie J. Sturzenbecker, Jeffrey J. Letourneau, Teresa Miller, Ilana L. Stroke, Maria L. Webb, Diana R. Savoly, David W. Hilbert, Linh Ma, Igor Pechik
Publikováno v:
Antimicrobial agents and chemotherapy. 62(5)
Clostridium difficile infection (CDI) is the leading cause of hospital-acquired infectious diarrhea, with significant morbidity, mortality, and associated health care costs. The major risk factor for CDI is antimicrobial therapy, which disrupts the n
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::46ab694a3cd02b2c6aab3e9bb9ef4ccd
https://pubmed.ncbi.nlm.nih.gov/29483125
https://pubmed.ncbi.nlm.nih.gov/29483125
Autor:
Steve Castro, Julie Clark, Amy Matheny, David M. Floyd, Philip D. Stein, Spencer Knapp, Gloria Holbrook, Martina Sigal, Fangyi Zhu, Senthil Krishnan, Michele Connelly, Jian Liu, Zheng Wang, Sridevi Bashyum, Rajkumar Dhinakaran, Jaeki Min, R. Kiplin Guy
Publikováno v:
Journal of medicinal chemistry. 59(17)
Phenotypic whole-cell screening in erythrocytic cocultures of Plasmodium falciparum identified a series of dihydroisoquinolones that possessed potent antimalarial activity against multiple resistant strains of P. falciparum in vitro and show no cytot
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7ddd8b1b44625739bf575e4ee09c7582
https://pubmed.ncbi.nlm.nih.gov/27505686
https://pubmed.ncbi.nlm.nih.gov/27505686
Autor:
Zheming Ruan, S. M. Seiler, Herbert E. Klei, Jing Zhang, Jeffrey A. Robl, Stephen P. O'connor, Mengxiao Shi, Liang Schweizer, John E. Macor, R. Michael Lawrence, Karnail S. Atwal, William A. Schumacher, Eddie C.-K. Liu, Sharon N. Bisaha, Doree F. Sitkoff, Ying Wang, Chi Li, Thomas E. Steinbacher, Yan Shi, Philip D. Stein, Kevin Kish
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:7516-7521
The design, synthesis and SAR of a novel class of valerolactam-based arylsulfonamides as potent and selective FXa inhibitors is reported. The arylsulfonamide-valerolactam scaffold was derived based on the proposed bioisosterism to the arylcyanoguanid
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::85bb84aabdb3a646b55d279059af6aab
https://doi.org/10.1016/j.bmcl.2011.06.098
https://doi.org/10.1016/j.bmcl.2011.06.098
Autor:
Joseph Yanchunas, Eddie C.-K. Liu, Christine Huang, S. M. Seiler, Yan Shi, Ying Wang, Karnail S. Atwal, Thomas E. Steinbacher, Doree F. Sitkoff, Andrew T. Pudzianowski, William A. Schumacher, Karen S. Hartl, Sharon N. Bisaha, Chi Li, Stephen P. O'connor, Kevin Kish, Mengxiao Shi, Philip D. Stein, Herbert E. Klei, Jing Zhang
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:6882-6889
We report the design and synthesis of a novel class of N,N'-disubstituted aroylguanidine-based lactam derivatives as potent and orally active FXa inhibitors. The structure-activity relationships (SAR) investigation led to the discovery of the nicotin
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0f30912ce064e83f0929d53206bf34b3
https://doi.org/10.1016/j.bmcl.2009.10.084
https://doi.org/10.1016/j.bmcl.2009.10.084
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b90d3adf6a8d7ca839916f3bce8ae5a0
https://doi.org/10.1021/jm800001n
https://doi.org/10.1021/jm800001n
Autor:
Wei Han, Patrick Y.S. Lam, Philip D. Stein, John E. Macor, Jing Zhang, Robert Zahler, Eddie C.-K. Liu, Karnail S. Atwal, Yan Shi, Ying Wang, Saleem Ahmad, Lawrence J. Kennedy, Stephen P. O'connor, S. M. Seiler, Jeffrey A. Robl, Zilun Hu, Doree F. Sitkoff
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:5952-5958
The design and synthesis of a novel class of amino(methyl) pyrrolidine-based sulfonamides as potent and selective FXa inhibitors is reported. The amino(methyl) pyrrolidine scaffolds were designed based on the proposed bioisosterism to the piperazine
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::10b9e6828f23d93787599d46256af2d5
https://doi.org/10.1016/j.bmcl.2007.07.063
https://doi.org/10.1016/j.bmcl.2007.07.063
Autor:
Adele M. Lehane, Anupam Pradhan, David A. Fidock, Dennis E. Kyle, Gloria Holbrook, Amy Matheny, Martina Sigal, Anang A. Shelat, David Waterson, Iñigo Angulo-Barturen, Kathleen O’Loughlin, Jian Liu, Laura M. Sanz, Philip D. Stein, Daniel H. Ebert, Kiaran Kirk, Hongshen Ma, Marcus C. S. Lee, Jon C. Mirsalis, W. Armand Guiguemde, Xiaoyan Deng, Greg Fedewa, Ane Rodríguez-Alejandre, María Belén Jiménez-Díaz, María G. Gómez, Angela K. Carrillo, Mariana Justino de Almeida, Yandira G. Salinas, Vicky M. Avery, David M. Shackleford, Sandra Duffy, Marie-Eve Myrand-Lapierre, Gregory M. Miller, María Santos Martínez, Adelaide S. M. Dennis, Charles C. Kim, R. Kiplin Guy, Julie Clark, Jeremy A. Horst, Aaron N. Endsley, Joseph L. DeRisi, Zheng Wang, Spencer Knapp, Fangyi Zhu, David M. Floyd, Santiago Ferrer, Jonathon Diep, Francisco-Javier Gamo, Susan A. Charman, Natalie J. Spillman
Publikováno v:
Proceedings of the National Academy of Sciences of the United States of America, vol 111, iss 50
Drug discovery for malaria has been transformed in the last 5 years by the discovery of many new lead compounds identified by phenotypic screening. The process of developing these compounds as drug leads and studying the cellular responses they induc
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bd38753b4b27787a1d271647ca26a4f8
https://europepmc.org/articles/PMC4273362/
https://europepmc.org/articles/PMC4273362/
Autor:
Jack Z. Gougoutas, Karen S. Hartl, R. Michael Lawrence, Doree F. Sitkoff, Gregory S. Bisacchi, Steven M. Seiler, Andrew T. Pudzianowski, William A. Schumacher, Philip D. Stein, Eddie C.-K. Liu, Thomas E. Steinbacher, Zhaoxiao Zhang, James C. Sutton
Publikováno v:
Letters in Drug Design & Discovery. 2:625-630
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::a7cee05c3fc0caebfd7b297901137ea0
https://doi.org/10.2174/157018005774717316
https://doi.org/10.2174/157018005774717316