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ID: ALA4425181

Journal: Bioorg Med Chem Lett

Title: Synthesis and antileishmanial activity of the core structure of cristaxenicin A.

Authors: Fumiyama H, Sadayuki T, Osada Y, Goto Y, Nakao Y, Hosokawa S.

Abstract: The core structure of cristaxenicin A having trans-fused dihydropyran and nine membered ring has been synthesized and evaluated the antileishmanial activity. The dihydropyran ring was synthesized by [4+2] cycloaddition reaction between an unsaturated aldehyde and a β-alkoxy-α,β-unsaturated ketone. The nine membered ring possessing α,β-unsaturated aldehyde was constructed by the intramolecular NHK reaction followed by the Mitsunobu rearrangement. The racemic core structure of cristaxenicin A was evaluated the anti-leishmanial activity with an IC50 value of 2.4μM.

CiteXplore: 27476143

DOI: 10.1016/j.bmcl.2016.06.061