Lisa Vieider, Erik Romp, Veronika Temml, Jana Fischer, Christian Kretzer, Martin Schönthaler, Abdulla Taha, Victor Hernández-Olmos, Sonja Sturm, Daniela Schuster, Oliver Werz, Ulrike Garscha, Barbara Matuszczak
- A series of derivatives of the potent dual soluble epoxide hydrolase (sEH)/5-lipoxygenase-activating protein (FLAP) inhibitor diflapolin was designed, synthesized, and characterized by 1H NMR, 13C NMR, and elemental analysis. These novel compounds were biologically evaluated for their inhibitory activity against sEH and FLAP. Molecular modeling tools were applied to analyze structure–activity relationships (SAR) on both targets. Results show that even small modifications on the lead compound diflapolin markedly influence the inhibitory potential, especially on FLAP, suggesting very narrow SAR.
Metadaten| Author: | Lisa Vieider, Erik Romp, Veronika Temml, Jana Fischer, Christian Kretzer, Martin Schönthaler, Abdulla Taha, Victor Hernández-OlmosORCiD, Sonja Sturm, Daniela SchusterORCiD, Oliver WerzORCiDGND, Ulrike Garscha, Barbara MatuszczakORCiD |
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| URN: | urn:nbn:de:hebis:30:3-488432 |
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| DOI: | https://doi.org/10.1021/acsmedchemlett.8b00415 |
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| ISSN: | 1948-5875 |
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| Pubmed Id: | https://pubmed.ncbi.nlm.nih.gov/30655948 |
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| Parent Title (English): | ACS medicinal chemistry letters |
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| Publisher: | ACS |
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| Place of publication: | Washington, DC |
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| Document Type: | Article |
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| Language: | English |
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| Year of Completion: | 2018 |
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| Date of first Publication: | 2018/11/29 |
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| Publishing Institution: | Universitätsbibliothek Johann Christian Senckenberg |
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| Release Date: | 2019/01/24 |
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| Tag: | 5-Lipoxygenase activating protein (FLAP); Arachidonic acid cascade; Diflapolin; Inflammation; Soluble epoxide hydrolase (sEH) |
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| Volume: | 10 |
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| Issue: | 1 |
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| Page Number: | 5 |
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| First Page: | 62 |
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| Last Page: | 66 |
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| Note: | ACS AuthorChoice - This is an open access article published under an ACS AuthorChoice License, which permits copying and redistribution of the article or any adaptations for non-commercial purposes. |
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| HeBIS-PPN: | 446286168 |
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| Institutes: | Biochemie, Chemie und Pharmazie / Pharmazie |
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| Dewey Decimal Classification: | 6 Technik, Medizin, angewandte Wissenschaften / 61 Medizin und Gesundheit / 610 Medizin und Gesundheit |
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| Sammlungen: | Universitätspublikationen |
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| Licence (English): |  Creative Commons - Namensnennung-Nicht kommerziell 4.0 |
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Creative Commons - Namensnennung-Nicht kommerziell 4.0