Chemical modification and structure-activity relationships of pyripyropenes; potent, bioavailable inhibitor of acyl-CoA: Cholesterol O-acyltransferase (ACAT)

Rika Obata; Toshiaki Sunazuka; Hiroshi Tomoda; Yoshihiro Harigaya; Satoshi Omura

doi:10.1016/0960-894X(95)00451-X

Chemical modification and structure-activity relationships of pyripyropenes; potent, bioavailable inhibitor of acyl-CoA: Cholesterol O-acyltransferase (ACAT)

Rika Obata, Toshiaki Sunazuka, Hiroshi Tomoda, Yoshihiro Harigaya, Satoshi Omura

人文社会学科

研究成果: Article › 査読

32 被引用数 (Scopus)

抄録

Modification and structure-activity relationships of ACAT inhibitor pyripyropene were examined. PR-109 (7g) showed the most potent (IC₅₀ = 6 nM) inhibitory activity. PR-86 (2e) also had strong inhibitory activity (IC₅₀ = 19 nM) and its in vivo activity improved 10 times better (ED₅₀ = 10 mg/kg) than that of pyripyropene A.

本文言語	English
ページ（範囲）	2683-2688
ページ数	6
ジャーナル	Bioorganic and Medicinal Chemistry Letters
巻	5
号	22
DOI	https://doi.org/10.1016/0960-894X(95)00451-X
出版ステータス	Published - 1995 11月 16

ASJC Scopus subject areas

生化学
分子医療
分子生物学
薬科学
創薬
臨床生化学
有機化学

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10.1016/0960-894X(95)00451-X

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引用スタイル

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author = "Rika Obata and Toshiaki Sunazuka and Hiroshi Tomoda and Yoshihiro Harigaya and Satoshi Omura",

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