Benzofuran and pyrrole derivatives as cannabinoid receptor modulators with in vivo efficacy against ulcerative colitis
Aim: Highlighting the need for effective therapies for the treatment of ulcerative colitis, novel series of potential CB2 modulators (benzofuran and pyrrole carboxamides) were developed and tested for their functional activities on CB1/CB2 receptors. Results: In the benzofuran series, the cannabinoid (CB) receptor selectivity and the functional profile were dependent on the nature of the amide substituent and the position of the methoxy group, meanwhile the pyrrole derivatives, displayed an exclusive selectivity to the CB2 receptor and a functionality that is controlled by the nature of the pyrrole nitrogen substituent. Conclusion: Remarkably, we succeeded to develop potent and selective pyrrole-based CB2 receptor agonists, represented by compound 25a, which also demonstrated an exquisite anti-inflammatory effect in a dextran sodium sulfate-induced colitis model in mice.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2019 |
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| Erschienen: |
2019 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:11 |
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| Enthalten in: |
Future medicinal chemistry - 11(2019), 24 vom: 21. Dez., Seite 3139-3159 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Wadea, Noura E [VerfasserIn] |
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| Links: |
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| Themen: |
Anti-Ulcer Agents |
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| Anmerkungen: |
Date Completed 10.07.2020 Date Revised 10.07.2020 published: Print Citation Status MEDLINE |
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| doi: |
10.4155/fmc-2019-0172 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM304399671 |
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| 100 | 1 | |a Wadea, Noura E |e verfasserin |4 aut | |
| 245 | 1 | 0 | |a Benzofuran and pyrrole derivatives as cannabinoid receptor modulators with in vivo efficacy against ulcerative colitis |
| 264 | 1 | |c 2019 | |
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| 500 | |a Date Completed 10.07.2020 | ||
| 500 | |a Date Revised 10.07.2020 | ||
| 500 | |a published: Print | ||
| 500 | |a Citation Status MEDLINE | ||
| 520 | |a Aim: Highlighting the need for effective therapies for the treatment of ulcerative colitis, novel series of potential CB2 modulators (benzofuran and pyrrole carboxamides) were developed and tested for their functional activities on CB1/CB2 receptors. Results: In the benzofuran series, the cannabinoid (CB) receptor selectivity and the functional profile were dependent on the nature of the amide substituent and the position of the methoxy group, meanwhile the pyrrole derivatives, displayed an exclusive selectivity to the CB2 receptor and a functionality that is controlled by the nature of the pyrrole nitrogen substituent. Conclusion: Remarkably, we succeeded to develop potent and selective pyrrole-based CB2 receptor agonists, represented by compound 25a, which also demonstrated an exquisite anti-inflammatory effect in a dextran sodium sulfate-induced colitis model in mice | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a CB modulators | |
| 650 | 4 | |a CB2 agonist | |
| 650 | 4 | |a DSS-induced colitis | |
| 650 | 4 | |a IBD | |
| 650 | 4 | |a benzofuran | |
| 650 | 4 | |a cannabinoid receptors | |
| 650 | 4 | |a pyrrole | |
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| 650 | 7 | |a Benzofurans |2 NLM | |
| 650 | 7 | |a Cannabinoid Receptor Agonists |2 NLM | |
| 650 | 7 | |a Pyrroles |2 NLM | |
| 650 | 7 | |a Receptor, Cannabinoid, CB2 |2 NLM | |
| 700 | 1 | |a Issac, Maro M |e verfasserin |4 aut | |
| 700 | 1 | |a Osman, Noha A |e verfasserin |4 aut | |
| 700 | 1 | |a Abadi, Ashraf H |e verfasserin |4 aut | |
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