Zobrazeno 1 - 10
of 30
pro vyhledávání: '"Michael N. Gwynn"'
Autor:
Graham Elgin Jones, Alan Joseph Hennessy, Steve Rittenhouse, Ilaria Giordano, Roger Edward Markwell, Steven Dabbs, Michael N. Gwynn, David T. Davies, Jennifer Hoover, Nathalie Cailleau, Barry S. Brown, Joel Michael Esken, Neil D. Pearson, Pamela Brown, Dongzhao Chen, Elisabeth A. Minthorn, Ben Bax, Gerald Brooks, Timothy J. Miles, Senthill K. Kusalakumari Sukmar
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 26:2464-2469
During the course of our research on the lead optimisation of the NBTI (Novel Bacterial Type II Topoisomerase Inhibitors) class of antibacterials, we discovered a series of tricyclic compounds that showed good Gram-positive and Gram-negative potency.
Autor:
Michael N. Gwynn, Jianzhong Huang, Martin Hibbs, Claus Spitzfaden, Jason Pizzollo, Haifeng Cui, Velupillai Srikannathasan, Robert Tanner, Karen A. Ingraham, Robert A. Stavenger, Pan F. Chan, Minghua Gu, Carol Shen, Paul Homes, Andrew J. Theobald, Andrew P. Fosberry, Anthony Shillings, Michael M. Hann, Benjamin D. Bax
Publikováno v:
Nature Communications
New antibacterials are needed to tackle antibiotic-resistant bacteria. Type IIA topoisomerases (topo2As), the targets of fluoroquinolones, regulate DNA topology by creating transient double-strand DNA breaks. Here we report the first co-crystal struc
Autor:
Pamela Brown, Roger Edward Markwell, David L. Downie, Susanne Eyrisch, Neil D. Pearson, Dongzhao Chen, Christopher Barfoot, Stephen Rittenhouse, Graham Elgin Jones, Mark A. Seefeld, Elizabeth A. Minthorn, Jeffrey M. Axten, Steven Dabbs, Alan Joseph Hennessy, Michael N. Gwynn, Gerald Brooks, Jianzhong Huang, Ilaria Giordano, William H. Miller, David T. Davies, Timothy Francis Gallagher, Timothy J. Miles, Jennifer Hoover
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:7489-7495
We have identified a series of amino-piperidine antibacterials with a good broad spectrum potency. We report the investigation of various subunits in this series and advanced studies on compound 8. Compound 8 possesses good pharmacokinetics, broad sp
Autor:
Stephen Rittenhouse, Neil D. Pearson, Christopher Barfoot, Graham Elgin Jones, Timothy J. Miles, David L. Downie, Dongzhao Chen, Steven Dabbs, Jennifer Hoover, Roger Edward Markwell, Alan Joseph Hennessy, Jianzhong Huang, Michael N. Gwynn, Ilaria Giordano, Gerald Brooks, Hong Xiang, David T. Davies, Susanne Eyrisch, Pamela Brown
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:7483-7488
As part of our wider efforts to exploit novel mode of action antibacterials, we have discovered a series of cyclohexyl-amide compounds that has good Gram positive and Gram negative potency. The mechanism of action is via inhibition of bacterial topoi
Publikováno v:
Annals of the New York Academy of Sciences. 1213:5-19
The discovery of novel antibiotic classes has not kept pace with the growing threat of bacterial resistance. Antibiotic candidates that act at new targets or via distinct mechanisms have the greatest potential to overcome resistance; however, novel a
Autor:
Claus Spitzfaden, Paul Homes, Andrew P. Fosberry, Jianzhong Huang, Martin Hibbs, Michael N. Gwynn, Anthony Shillings, Alexandre Wohlkonig, Andrew J. Theobald, Pan F. Chan, Velupillai Srikannathasan, Onkar M. P. Singh, Benjamin D. Bax
Fluoroquinolone drugs such as moxifloxacin kill bacteria by stabilizing the normally transient double-stranded DNA breaks created by bacterial type IIA topoisomerases. Previous crystal structures of Staphylococcus aureus DNA gyrase with asymmetric DN
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ab10eeb8df12cca74374d1610c9aeae7
https://hdl.handle.net/20.500.14017/22db32c0-99c6-4908-a958-7283af6f9d72
https://hdl.handle.net/20.500.14017/22db32c0-99c6-4908-a958-7283af6f9d72
Autor:
Linda A. Miller, Michael J. Italia, Michael N. Gwynn, Julie A. Becker, Heather Amrine-Madsen, Michael J. Stanhope, Tom Mathie, J. A. Poupard, Stacey L. Walsh, Karen A. Ingraham, James R. Brown
Publikováno v:
Antimicrobial Agents and Chemotherapy. 49:4315-4326
Fluoroquinolones are an important class of antibiotics for the treatment of infections arising from the gram-positive respiratory pathogen Streptococcus pneumoniae . Although there is evidence supporting interspecific lateral DNA transfer of fluoroqu
Autor:
Michael N. Gwynn, Martin Rosenberg, Nino Campobasso, Howard Kallender, Mehul Patel, Imogen E. Wilding
Publikováno v:
Journal of Biological Chemistry. 279:44883-44888
3-Hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) synthase, a member of the family of acyl-condensing enzymes, catalyzes the first committed step in the mevalonate pathway and is a potential target for novel antibiotics and cholesterol-lowering agents.
Publikováno v:
Journal of Biological Chemistry. 278:8861-8868
Type II topoisomerases bind to DNA at the catalytic domain across the DNA gate. DNA gyrases also bind to DNA at the non-homologous C-terminal domain of the GyrA subunit, which causes the wrapping of DNA about itself. This unique mode of DNA binding a
Autor:
Cynthia V. Stauffacher, John W. Burgner, Autumn Sutherlin, Kevin R. Lehnbeuter, E. Imogen Wilding, Victor W. Rodwell, Damien McDevitt, Marie J. Mazzulla, Pamela Lane, Michael N. Gwynn, Matija Hedl
Publikováno v:
Bindley Publications
Many bacteria employ the nonmevalonate pathway for synthesis of isopentenyl diphosphate, the monomer unit for isoprenoid biosynthesis. However, gram-positive cocci exclusively use the mevalonate pathway, which is essential for their growth (E. I. Wil