ArticleOrganic letters2026
Liquid-Phase Peptide Synthesis of Tropolone-Peptide Hybrid Antimalarials.
Article in Organic letters, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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Authors and funding
9 authors.
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Abstract
Tropolones are non-benzenoid aromatics with broad bioactivity, yet their inherent planarity and metal-chelating properties pose challenges to a medicinal chemistry campaign. We developed a liquid-phase peptide synthesis strategy that leveraged a hydrophobic TAG carrier to streamline condensation, deprotection, and purification steps, overcoming challenges that hinder traditional solution-phase derivatization of tropolones. Among the synthesized tropolone-peptide hybrid derivatives, the lead analogue exceeded antimalarial potency of puberulic acid and artemisinin, highlighting the advantage of three-dimensional peptide hybridization.
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