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脂肪积累抑制剂(-)-ternatin的整体构效关系:认识每个氨基酸残基的重要性。

Whole structure-activity relationships of the fat-accumulation inhibitor (-)-ternatin: recognition of the importance of each amino acid residue.

作者信息

Shimokawa Kenichiro, Iwase Yoshiaki, Miwa Ryoka, Yamada Kaoru, Uemura Daisuke

机构信息

Department of Chemistry, Graduate School of Science, Nagoya University, Furo-cho, Chikusa, Nagoya 464-8602, Japan.

出版信息

J Med Chem. 2008 Oct 9;51(19):5912-4. doi: 10.1021/jm800741n. Epub 2008 Sep 18.

Abstract

A series of Ala and Aoc analogues of (-)-ternatin were prepared, and their bioactivities were assessed by a fat-accumulation inhibition assay using 3T3-L1 adipocytes, which led to the discovery of key structure-activity relationships (SAR).

摘要

制备了一系列(-)-ternatin的丙氨酸(Ala)和鹅肌肽(Aoc)类似物,并通过使用3T3-L1脂肪细胞的脂肪积累抑制试验评估了它们的生物活性,从而发现了关键的构效关系(SAR)。

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