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2- and 3-substituted imidazo[1,2-a]pyrazines as inhibitors of bacterial type IV secretion
A novel series of 8-amino imidazo[1,2-a]pyrazine derivatives has been developed as inhibitors of the VirB11 ATPase HP0525, a key component of the bacterial type IV secretion system. A flexible synthetic route to both 2- and 3-aryl substituted regioisomers has been developed. The resulting series of...
| Autores principales: | , , , , , , , , , , , |
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| Formato: | Online Artículo Texto |
| Lenguaje: | English |
| Publicado: |
Elsevier Science
2014
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| Materias: | |
| Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4339681/ https://www.ncbi.nlm.nih.gov/pubmed/25438770 http://dx.doi.org/10.1016/j.bmc.2014.09.036 |
| _version_ | 1782358898590613504 |
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| author | Sayer, James R. Walldén, Karin Pesnot, Thomas Campbell, Frederick Gane, Paul J. Simone, Michela Koss, Hans Buelens, Floris Boyle, Timothy P. Selwood, David L. Waksman, Gabriel Tabor, Alethea B. |
| author_facet | Sayer, James R. Walldén, Karin Pesnot, Thomas Campbell, Frederick Gane, Paul J. Simone, Michela Koss, Hans Buelens, Floris Boyle, Timothy P. Selwood, David L. Waksman, Gabriel Tabor, Alethea B. |
| author_sort | Sayer, James R. |
| collection | PubMed |
| description | A novel series of 8-amino imidazo[1,2-a]pyrazine derivatives has been developed as inhibitors of the VirB11 ATPase HP0525, a key component of the bacterial type IV secretion system. A flexible synthetic route to both 2- and 3-aryl substituted regioisomers has been developed. The resulting series of imidazo[1,2-a]pyrazines has been used to probe the structure–activity relationships of these inhibitors, which show potential as antibacterial agents. |
| format | Online Article Text |
| id | pubmed-4339681 |
| institution | National Center for Biotechnology Information |
| language | English |
| publishDate | 2014 |
| publisher | Elsevier Science |
| record_format | MEDLINE/PubMed |
| spelling | pubmed-43396812015-03-03 2- and 3-substituted imidazo[1,2-a]pyrazines as inhibitors of bacterial type IV secretion Sayer, James R. Walldén, Karin Pesnot, Thomas Campbell, Frederick Gane, Paul J. Simone, Michela Koss, Hans Buelens, Floris Boyle, Timothy P. Selwood, David L. Waksman, Gabriel Tabor, Alethea B. Bioorg Med Chem Article A novel series of 8-amino imidazo[1,2-a]pyrazine derivatives has been developed as inhibitors of the VirB11 ATPase HP0525, a key component of the bacterial type IV secretion system. A flexible synthetic route to both 2- and 3-aryl substituted regioisomers has been developed. The resulting series of imidazo[1,2-a]pyrazines has been used to probe the structure–activity relationships of these inhibitors, which show potential as antibacterial agents. Elsevier Science 2014-11-15 /pmc/articles/PMC4339681/ /pubmed/25438770 http://dx.doi.org/10.1016/j.bmc.2014.09.036 Text en © 2014 The Authors https://creativecommons.org/licenses/by/3.0/This work is licensed under a Creative Commons Attribution 3.0 Unported License (https://creativecommons.org/licenses/by/3.0/) . |
| spellingShingle | Article Sayer, James R. Walldén, Karin Pesnot, Thomas Campbell, Frederick Gane, Paul J. Simone, Michela Koss, Hans Buelens, Floris Boyle, Timothy P. Selwood, David L. Waksman, Gabriel Tabor, Alethea B. 2- and 3-substituted imidazo[1,2-a]pyrazines as inhibitors of bacterial type IV secretion |
| title | 2- and 3-substituted imidazo[1,2-a]pyrazines as inhibitors of bacterial type IV secretion |
| title_full | 2- and 3-substituted imidazo[1,2-a]pyrazines as inhibitors of bacterial type IV secretion |
| title_fullStr | 2- and 3-substituted imidazo[1,2-a]pyrazines as inhibitors of bacterial type IV secretion |
| title_full_unstemmed | 2- and 3-substituted imidazo[1,2-a]pyrazines as inhibitors of bacterial type IV secretion |
| title_short | 2- and 3-substituted imidazo[1,2-a]pyrazines as inhibitors of bacterial type IV secretion |
| title_sort | 2- and 3-substituted imidazo[1,2-a]pyrazines as inhibitors of bacterial type iv secretion |
| topic | Article |
| url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4339681/ https://www.ncbi.nlm.nih.gov/pubmed/25438770 http://dx.doi.org/10.1016/j.bmc.2014.09.036 |
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