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  • Title: Chemical modification and structure-activity relationships of pyripyropenes. 2. 1,11-Cyclic analogs.
    Author: Obata R, Sunazuka T, Kato Y, Tomoda H, Harigaya Y, Omura S.
    Journal: J Antibiot (Tokyo); 1996 Nov; 49(11):1149-56. PubMed ID: 8982344.
    Abstract:
    A series of 1,11-cyclic analogs of pyripyropene A were prepared. Replacement of the 1,11-acyl groups of pyripyropenes with 1,11-cyclic acetals effectively improved in vitro acyl CoA:cholesterol acyltransferase (ACAT) inhibitory activity. Especially noteworthy is benzylidene acetal analog 35, the most potent inhibitor (IC50 = 5.6 nM) among the derivatives prepared so far, which showed 16 times more potent inhibitory activity than pyripyropene A.
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