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Practical Synthesis and Application of Halogen-Doped Pyrrole Building Blocks
[Image: see text] A practical access to four new halogen-substituted pyrrole building blocks was realized in two to five synthetic steps from commercially available starting materials. The target compounds were prepared on a 50 mg to 1 g scale, and their conversion to nanomolar inhibitors of bacteri...
| Autores principales: | , , , , , , , , , , , , , , , , |
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| Formato: | Online Artículo Texto |
| Lenguaje: | English |
| Publicado: |
American Chemical Society
2021
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| Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8047689/ https://www.ncbi.nlm.nih.gov/pubmed/33869952 http://dx.doi.org/10.1021/acsomega.1c00331 |
| _version_ | 1783679090351407104 |
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| author | Cotman, Andrej Emanuel Guérin, Thomas Kovačević, Ivana Benedetto Tiz, Davide Durcik, Martina Fulgheri, Federica Možina, Štefan Secci, Daniela Sterle, Maša Ilaš, Janez Zega, Anamarija Zidar, Nace Mašič, Lucija Peterlin Tomašič, Tihomir Leroux, Frédéric R. Hanquet, Gilles Kikelj, Danijel |
| author_facet | Cotman, Andrej Emanuel Guérin, Thomas Kovačević, Ivana Benedetto Tiz, Davide Durcik, Martina Fulgheri, Federica Možina, Štefan Secci, Daniela Sterle, Maša Ilaš, Janez Zega, Anamarija Zidar, Nace Mašič, Lucija Peterlin Tomašič, Tihomir Leroux, Frédéric R. Hanquet, Gilles Kikelj, Danijel |
| author_sort | Cotman, Andrej Emanuel |
| collection | PubMed |
| description | [Image: see text] A practical access to four new halogen-substituted pyrrole building blocks was realized in two to five synthetic steps from commercially available starting materials. The target compounds were prepared on a 50 mg to 1 g scale, and their conversion to nanomolar inhibitors of bacterial DNA gyrase B was demonstrated for three of the prepared building blocks to showcase the usefulness of such chemical motifs in medicinal chemistry. |
| format | Online Article Text |
| id | pubmed-8047689 |
| institution | National Center for Biotechnology Information |
| language | English |
| publishDate | 2021 |
| publisher | American Chemical Society |
| record_format | MEDLINE/PubMed |
| spelling | pubmed-80476892021-04-16 Practical Synthesis and Application of Halogen-Doped Pyrrole Building Blocks Cotman, Andrej Emanuel Guérin, Thomas Kovačević, Ivana Benedetto Tiz, Davide Durcik, Martina Fulgheri, Federica Možina, Štefan Secci, Daniela Sterle, Maša Ilaš, Janez Zega, Anamarija Zidar, Nace Mašič, Lucija Peterlin Tomašič, Tihomir Leroux, Frédéric R. Hanquet, Gilles Kikelj, Danijel ACS Omega [Image: see text] A practical access to four new halogen-substituted pyrrole building blocks was realized in two to five synthetic steps from commercially available starting materials. The target compounds were prepared on a 50 mg to 1 g scale, and their conversion to nanomolar inhibitors of bacterial DNA gyrase B was demonstrated for three of the prepared building blocks to showcase the usefulness of such chemical motifs in medicinal chemistry. American Chemical Society 2021-03-30 /pmc/articles/PMC8047689/ /pubmed/33869952 http://dx.doi.org/10.1021/acsomega.1c00331 Text en © 2021 The Authors. Published by American Chemical Society Permits the broadest form of re-use including for commercial purposes, provided that author attribution and integrity are maintained (https://creativecommons.org/licenses/by/4.0/). |
| spellingShingle | Cotman, Andrej Emanuel Guérin, Thomas Kovačević, Ivana Benedetto Tiz, Davide Durcik, Martina Fulgheri, Federica Možina, Štefan Secci, Daniela Sterle, Maša Ilaš, Janez Zega, Anamarija Zidar, Nace Mašič, Lucija Peterlin Tomašič, Tihomir Leroux, Frédéric R. Hanquet, Gilles Kikelj, Danijel Practical Synthesis and Application of Halogen-Doped Pyrrole Building Blocks |
| title | Practical Synthesis and Application of Halogen-Doped
Pyrrole Building Blocks |
| title_full | Practical Synthesis and Application of Halogen-Doped
Pyrrole Building Blocks |
| title_fullStr | Practical Synthesis and Application of Halogen-Doped
Pyrrole Building Blocks |
| title_full_unstemmed | Practical Synthesis and Application of Halogen-Doped
Pyrrole Building Blocks |
| title_short | Practical Synthesis and Application of Halogen-Doped
Pyrrole Building Blocks |
| title_sort | practical synthesis and application of halogen-doped
pyrrole building blocks |
| url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8047689/ https://www.ncbi.nlm.nih.gov/pubmed/33869952 http://dx.doi.org/10.1021/acsomega.1c00331 |
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