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. 2007 Mar 15;17(6):1544-8.
doi: 10.1016/j.bmcl.2006.12.100. Epub 2007 Jan 8.

In vitro antimalarial activity of hyperforin, a prenylated acylphloroglucinol. A structure-activity study

Luisella Verotta  1 , Giovanni Appendino, Ezio Bombardelli, Reto Brun
Affiliations

In vitro antimalarial activity of hyperforin, a prenylated acylphloroglucinol. A structure-activity study

Luisella Verotta et al. Bioorg Med Chem Lett. .

Abstract

The antimalarial activity of hyperforin, a phenol-like compound that can be easily absorbed orally, and a series of derivatives variously modified on the cyclohexatrienone system was investigated. Hyperforin was active against Plasmodium falciparum with an IC(50) value in the micromolar range, and the activity was not critically dependent on either its phenol-like sensitivity to autooxidation or the presence of unsaturation on the prenyl residues. Related phloroglucinols like the hop beta-acids and the enantiomers of usnic acid showed only marginal activity, suggesting that hyperforin is a new antimalarial chemotype.

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