Zobrazeno 1 - 10
of 17
pro vyhledávání: '"Linda E. Chovan"'
Autor:
Linda E. Chovan, Peter J. Dandliker, Prisca Honore, Jennifer A. Garton, Yau Yi Lau, Andrew O. Stewart, Robert B. Moreland, Jorge D. Brioni, Frank L. Wagenaar, Odile F. El Kouhen, Teodozyi Kolasa, Xueqing Wang, Candace L. Black-Shaefer
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:4303-4307
Our HTS effort yielded a preferential mGluR1 pyrimidinone antagonist 1 with lead-like characteristics. Rapid hit to lead (HTL) study identified compounds with improved functional activity and selectivity such as 1b with little improvements in ADME pr
Autor:
Larry L. Klein, Teresa M Turner, Hui-Ju Chen, Lisa E. Hernandez, John T. Randolph, Cheri Klein, Clinton M. Yeung, Kennan C. Marsh, Zhiwen Guan, Linda E. Chovan, Yau Y Lau, Dale J. Kempf, Peter J. Dandliker
Publikováno v:
Antiviral Chemistry and Chemotherapy. 18:163-167
Inhibitors of hepatitis C virus (HCV) protease have shown marked antiviral activity in short-term clinical studies in HCV-infected individuals. The interaction of the investigational HCV protease inhibitors VX-950 and SCH 503034 with ritonavir, a pot
Autor:
Tianyuan Zhang, Richard A. G. Smith, Rohinton Edalji, Yu-Gui Gu, John L. Baranowski, William J. Sanders, Bruce A. Beutel, Liping Yu, Philip J. Hajduk, Annapur Gurulingappa Shivakumar, Stephan J. Kakavas, Frank L. Wagenaar, Darlene J. Balli, Steven F. Betz, Richard F. Clark, Kenneth M. Comess, Eric J. Hebert, J. Owen McCall, Jamey Mack, Linda E. Chovan, Randy E. Metzger, Thomas F. Holzman, Anne Y. Saiki, Sarah A. Dorwin, Niru B. Soni, Mai Bui, Angela M. Nilius, Susan J. Thornewell, Cooper Curt S, Mark E. Schurdak, Michael L. Coen, Rolf Wagner, Alan S. Florjancic, Philip J. Merta, Claude G. Lerner, Charlotte Woodall, Candace Black-Schaefer, John E. Harlan, Mengli Cai, Karl A. Walter, Xenia B. Searle, Stephen W. Fesik
Publikováno v:
Chemical Biology & Drug Design. 69:395-404
As part of a fully integrated and comprehensive strategy to discover novel antibacterial agents, NMR- and mass spectrometry-based affinity selection screens were performed to identify compounds that bind to protein targets uniquely found in bacteria
Autor:
Hovis M. Imade, Jiahong Wang, Russell A. Judge, Steven Fung, Martin Winn, Peer B. Jacobson, Bryan K. Sorensen, William J. Chiou, DeAnne Stolarik, Michael E. Brune, Ernst U. Frevert, Wenying Qin, Kenton L. Longenecker, Katina Monzon, J.T. Link, Linda E. Chovan, Jeff Rohde, Xiaoqing Deng, Qi Shuai, Heidi S. Camp, Liping Pan
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:527-532
Potent and selective adamantane sulfone and sulfonamide inhibitors of 11-beta-HSD-1 have been discovered. Selected compounds from these series have robust pharmacokinetic profiles and strongly inhibit liver, fat, and brain HSD1 for extended periods a
Autor:
Hovis M. Imade, Hing L. Sham, Liping Pan, Linda E. Chovan, Heidi S. Camp, Bryan K. Sorensen, Rodger F. Henry, Jiahong Wang, Atul Ramaiya, Mark M. Mullally, Rohde Jeffrey J, J.T. Link, William J. Chiou, Katina Monzon, Peer B. Jacobson, Thomas A. Fey, Kennan C. Marsh, Xiaoqing Deng, David W A Beno, DeAnne Stolarik, Brian A. Droz, Steven Fung, Michael E. Brune, Ernst U. Frevert, Marina A. Pliushchev, Qi Shuai, Dariusz Wodka
Publikováno v:
Journal of Medicinal Chemistry. 50:149-164
Starting from a rapidly metabolized adamantane 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1) inhibitor 22a, a series of E-5-hydroxy-2-adamantamine inhibitors, exemplified by 22d and (+/-)-22f, was discovered. Many of these compounds are po
Autor:
Niru B. Soni, Rolf Wagner, Steve D. Pratt, Teresa A. Rosenberg, Linda E. Chovan, Darlene J. Balli, Candace Black-Schaefer, Angela M. Nilius, Philip J. Merta, Moshe Weitzberg, Mira M. Hinman, Bruce A. Beutel, Frank L. Wagenaar, Douglas Kalvin
Publikováno v:
Journal of Medicinal Chemistry. 49:4842-4856
We describe the synthesis and antibacterial activity of a series of tetracyclic naphthyridones. The members of this series act primarily via inhibition of bacterial translation and belong to the class of novel ribosome inhibitors (NRIs). In this pape
Autor:
Angela M. Nilius, Yu-Gui Gu, Tamara Rehm, Mai H. Bui, Peter J. Dandliker, Bruce A. Beutel, T. Matthew Hansen, Linda E. Chovan
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:2716-2719
A series of 5-methoxy- and 5-hydroxy-6-fluoro-1,8-naphthyridone-3-carboxylic acid derivatives were prepared and evaluated for cell-free bacterial protein synthesis inhibition and whole cell antibacterial activity. When compared to the analogous 5-hyd
Autor:
Richard F. Clark, Xiaoan Ruan, Xiaoling Xuei, Rolf Wagner, Ping Zhong, Caroline A. David, Steve D. Pratt, Moshe Weitzberg, Candace Black-Schaefer, Linus L. Shen, Peter J. Dandliker, Yingna Cai, Erika E. Englund, Stephan J. Kakavas, Angela M. Nilius, Niru B. Soni, Mai Bui, Melissa M. Daly, Philip J. Merta, Danli L. Towne, Bruce A. Beutel, Linda E. Chovan, Zhensheng Cao, Robert K. Hickman, Anne Y. Saiki, Claude G. Lerner
Publikováno v:
Antimicrobial Agents and Chemotherapy. 47:3831-3839
We report the discovery and characterization of a novel ribosome inhibitor (NRI) class that exhibits selective and broad-spectrum antibacterial activity. Compounds in this class inhibit growth of many gram-positive and gram-negative bacteria, includi
Autor:
Edward T. Olejniczak, Angelo Gunasekera, Xiaoan Ruan, Claude G. Lerner, Linda E. Chovan, Jamey Mack, Liping Yu, Stephen W. Fesik, Danli L. Towne
Publikováno v:
Journal of Molecular Biology. 311:593-604
Streptococcus pneumoniae is a major human pathogen that causes high mortality and morbidity rates and has developed resistance to many antibiotics. The genome of S. pneumoniae has recently been completely sequenced revealing many genes encoding hypot
Autor:
Dominique Aubert, Jeff Hunt, Linda E. Chovan, Gregory T. Maine, A. Beorchia, Michael Sheu, Henriette Burlet, A. Bonhomme, Michel Pluot, John Tyner, Lawrence V. Howard, Isabelle Villena, J. M. Pinon, Sue Brojanac
Publikováno v:
Journal of Histochemistry & Cytochemistry. 46:1411-1421
Ultrastructural localization of a P29 protein of Toxoplasma gondii was examined on thin sections by an immunogold technique using a P29 antigen-specific monoclonal antibody (5-241-178). Immunolocalization of the P29 protein in extracellular tachyzoit