Academic Journal
Structure–activity relationship investigation of triazole-based kappa opioid receptor agonists
| العنوان: | Structure–activity relationship investigation of triazole-based kappa opioid receptor agonists |
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| المؤلفون: | Frankowski, K.J., Brust, T., Lovell, K.M., Yoo, E., Bohn, L.M., Aubé, J. |
| المصدر: | Medicinal Chemistry Research, 30(7) |
| بيانات النشر: | Springer |
| سنة النشر: | 2021 |
| المجموعة: | Carolina Digital Repository (UNC - University of North Carolina) |
| مصطلحات موضوعية: | Kappa opioid receptor, Triazoles, Antinociceptive agents, Anti-itch agents, Opioids |
| الوصف: | Select triazole-based small molecules possess potent and selective kappa opioid receptor (KOR) agonism. Here, we designed twenty new analogs to investigate the structure–activity relationship effects for all three functional groups attached to the triazole core. We identified specific groups that are critical for KOR potency and further extended the range of moieties explored. These efforts revealed analogs with potency on par with our lead triazole probe molecule, Triazole 1.1, in addition to analogs possessing a spectrum of less potent KOR agonist activity. |
| نوع الوثيقة: | article in journal/newspaper |
| اللغة: | English |
| Relation: | https://doi.org/10.17615/h2e9-c541; https://cdr.lib.unc.edu/assets/work-ff055336041c3f7d310ad69109eda4a887b16ec501f35afc0a547c4adb97ee72.png |
| DOI: | 10.17615/h2e9-c541 |
| الاتاحة: | https://doi.org/10.17615/h2e9-c541 https://cdr.lib.unc.edu/assets/work-ff055336041c3f7d310ad69109eda4a887b16ec501f35afc0a547c4adb97ee72.png |
| Rights: | http://rightsstatements.org/vocab/InC/1.0/ |
| رقم الانضمام: | edsbas.6056B4F8 |
| قاعدة البيانات: | BASE |
| DOI: | 10.17615/h2e9-c541 |
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