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Peer-reviewed veterinary case report

Synthesis and biological evaluation of a focused library of beauveriolides.

Journal:
Bioorganic & medicinal chemistry letters
Year:
2008
Authors:
Nagai, Kenichiro et al.
Affiliation:
Kitasato Institute for Life Sciences and Graduate School of Infection Control Sciences · Japan

Abstract

Fungal beauveriolide III (1b), discovered as an inhibitor of lipid droplet accumulation in mouse macrophages and showing antiatherogenic activity in mouse model, consists of l-Phe, l-Ala, d-allo-Ile, and (3S, 4S)-3-hydroxy-4-methyloctanoic acid moieties. A combinatorial library of beauveriolide analogues focusing on l-Ala and d-allo-Ile of 1b was synthesized by combinatorial synthesis. Among them, d-Ala analogues consisting of A{2} improved their solubility, while those with 7{1,3,2},7{2,3,1}, and 7{2,3,2} were 20 times more potent than 1b.

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Original publication: https://pubmed.ncbi.nlm.nih.gov/18620856/