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Synthesis and structure–activity relationships for some novel diflapolin derivatives with benzimidazole subunit
A series of derivatives of the potent dual soluble epoxide hydrolase (sEH)/5-lipoxygenase-activating protein (FLAP) inhibitor diflapolin was designed, synthesised, and characterised. These novel compounds, which contain a benzimidazole subunit were evaluated for their inhibitory activity against sEH...
| Autores principales: | , , , , , , , , , , |
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| Formato: | Online Artículo Texto |
| Lenguaje: | English |
| Publicado: |
Taylor & Francis
2022
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| Materias: | |
| Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9518245/ https://www.ncbi.nlm.nih.gov/pubmed/36124840 http://dx.doi.org/10.1080/14756366.2022.2087645 |
| _version_ | 1784799136060538880 |
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| author | Vieider, Lisa Zoeller, Eva Romp, Erik Schoenthaler, Martin Hernández-Olmos, Victor Temml, Veronika Hasenoehrl, Thomas Schuster, Daniela Werz, Oliver Garscha, Ulrike Matuszczak, Barbara |
| author_facet | Vieider, Lisa Zoeller, Eva Romp, Erik Schoenthaler, Martin Hernández-Olmos, Victor Temml, Veronika Hasenoehrl, Thomas Schuster, Daniela Werz, Oliver Garscha, Ulrike Matuszczak, Barbara |
| author_sort | Vieider, Lisa |
| collection | PubMed |
| description | A series of derivatives of the potent dual soluble epoxide hydrolase (sEH)/5-lipoxygenase-activating protein (FLAP) inhibitor diflapolin was designed, synthesised, and characterised. These novel compounds, which contain a benzimidazole subunit were evaluated for their inhibitory activity against sEH and FLAP. Molecular modelling tools were applied to analyse structure–activity relationships (SAR) on both targets and to predict solubility and gastrointestinal (GI) absorption. The most promising dual inhibitors of these series are 5a, 6b, and 6c. |
| format | Online Article Text |
| id | pubmed-9518245 |
| institution | National Center for Biotechnology Information |
| language | English |
| publishDate | 2022 |
| publisher | Taylor & Francis |
| record_format | MEDLINE/PubMed |
| spelling | pubmed-95182452022-09-29 Synthesis and structure–activity relationships for some novel diflapolin derivatives with benzimidazole subunit Vieider, Lisa Zoeller, Eva Romp, Erik Schoenthaler, Martin Hernández-Olmos, Victor Temml, Veronika Hasenoehrl, Thomas Schuster, Daniela Werz, Oliver Garscha, Ulrike Matuszczak, Barbara J Enzyme Inhib Med Chem Research Paper A series of derivatives of the potent dual soluble epoxide hydrolase (sEH)/5-lipoxygenase-activating protein (FLAP) inhibitor diflapolin was designed, synthesised, and characterised. These novel compounds, which contain a benzimidazole subunit were evaluated for their inhibitory activity against sEH and FLAP. Molecular modelling tools were applied to analyse structure–activity relationships (SAR) on both targets and to predict solubility and gastrointestinal (GI) absorption. The most promising dual inhibitors of these series are 5a, 6b, and 6c. Taylor & Francis 2022-09-20 /pmc/articles/PMC9518245/ /pubmed/36124840 http://dx.doi.org/10.1080/14756366.2022.2087645 Text en © 2022 The Author(s). Published by Informa UK Limited, trading as Taylor & Francis Group. https://creativecommons.org/licenses/by/4.0/This is an Open Access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/4.0/ (https://creativecommons.org/licenses/by/4.0/) ), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. |
| spellingShingle | Research Paper Vieider, Lisa Zoeller, Eva Romp, Erik Schoenthaler, Martin Hernández-Olmos, Victor Temml, Veronika Hasenoehrl, Thomas Schuster, Daniela Werz, Oliver Garscha, Ulrike Matuszczak, Barbara Synthesis and structure–activity relationships for some novel diflapolin derivatives with benzimidazole subunit |
| title | Synthesis and structure–activity relationships for some novel diflapolin derivatives with benzimidazole subunit |
| title_full | Synthesis and structure–activity relationships for some novel diflapolin derivatives with benzimidazole subunit |
| title_fullStr | Synthesis and structure–activity relationships for some novel diflapolin derivatives with benzimidazole subunit |
| title_full_unstemmed | Synthesis and structure–activity relationships for some novel diflapolin derivatives with benzimidazole subunit |
| title_short | Synthesis and structure–activity relationships for some novel diflapolin derivatives with benzimidazole subunit |
| title_sort | synthesis and structure–activity relationships for some novel diflapolin derivatives with benzimidazole subunit |
| topic | Research Paper |
| url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9518245/ https://www.ncbi.nlm.nih.gov/pubmed/36124840 http://dx.doi.org/10.1080/14756366.2022.2087645 |
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