Structure–activity relationship investigation of triazole-based kappa opioid receptor agonists

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  • April 22, 2022
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  • Frankowski, K.J.
    • Eshelman School of Pharmacy, Center for Integrative Chemical Biology and Drug Discovery
  • Brust, T.
    • Other Affiliation: The Scripps Research Institute
  • Lovell, K.M.
    • Other Affiliation: The Scripps Research Institute
  • Yoo, E.
    • Other Affiliation: University of Kansas
  • Bohn, L.M.
    • Other Affiliation: The Scripps Research Institute
  • Aubé, J.
    • Eshelman School of Pharmacy, Center for Integrative Chemical Biology and Drug Discovery
Abstract
  • 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.
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  • English

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