Acetoxybenzhydrols as highly active and stable analogues of 1′S

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• 作者：Tomohisa Yasuhara ; Yoshiaki Manse ; Takayuki Morimoto ; Wang Qilong ; Hisashi Matsuda ; Masayuki Yoshikawa ; Osamu Muraoka
• 关键词：Acetoxychavicol acetate ; Type I antiallergic activity ; Alpinia galanga
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2009
• 出版时间：1 June 2009
• 年：2009
• 卷：19
• 期：11
• 页码：2944-2946
• 全文大小：373 K

文摘

Through SAR studies on 1′S-1′-acetoxychavicol acetate (1) against Type I antiallergic activity by indexing release of β-hexosaminidase, a marker of antigen-IgE-mediated degranulation in RBL-2H3 cells, more stable and potent analogue, 4-(methoxycarbonyloxyphenylmethyl)phenyl acetate (16), has been developed. The compound 16 also strongly inhibited the antigen-IgE-mediated TNF-α and IL-4 production.