摘要:
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. (c) 2008 Elsevier Ltd. All rights reserved.