抄録
Four hydroxyl groups of pyripyropenes have been modified and evaluated for their ability to inhibit microsomal acyl-CoA: cholesterol acyltransferase (ACAT) activity in vitro and to lower cholesterol absorption in vivo in a cholesterol-fed hamster. 7-O-n-Valeryl derivative (8c) improved the in vitro ACAT inhibitory activity (IC50 = 13 nM) about 7 times better than pyripyropene A. Introduction of methanesulfonyl group at 11-hydroxyl group (17a) increased both in vitro activity(IC50 = 19 nM) and in vivo efficacy (ED50 = 10 mg/kg).
本文言語 | English |
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ページ(範囲) | 1133-1148 |
ページ数 | 16 |
ジャーナル | Journal of Antibiotics |
巻 | 49 |
号 | 11 |
DOI | |
出版ステータス | Published - 1996 |
ASJC Scopus subject areas
- 薬理学
- 創薬