Discovery of 1,2,3-triazole-based fibroblast growth factor receptor modulators.

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ID: 1868
2019
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Ranked #11 of 246 articles by views in Bioorganic & medicinal chemistry letters

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Abstract
To avoid production of a phospholipidosis-inducing metabolite, we replaced the amide structure of SUN13837 (1) with a 1,2,3-triazole. The resulting 1,2,3-triazole analog of 1 (compound 2) displayed greater neuroprotective activity than 1. Structural modification of 2 yielded compound 10, which showed improved neuroprotective activity and negligible mechanism-based inactivation against CYP3A4. In addition, installation of a methyl group at the 5-position of 1,2,3-triazole of 10 significantly boosted the neuroprotective activity. These 1,2,3-triazole derivatives displayed reduced phospholipidosis risk, sufficient systemic exposure, and high central nervous system penetration, and therefore may be potentially useful agents for the treatment of neurodegenerative diseases.
Reference Key
sakai2019discoverybioorganic Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors Sakai, Hiroki;Inoue, Hidekazu;Toba, Tetsuya;Murata, Kenji;Narii, Nobuhiro;Shimmyo, Yoshiari;Igawa, Yoshiyuki;Matsumoto, Takahiro;Takemoto, Naohiro;
Journal Bioorganic & medicinal chemistry letters
Year 2019
DOI
S0960-894X(19)30396-8
URL
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