Furuta Takumi, Hirooka Yasuo, Abe Ayako, Sugata Yusuke, Ueda Mitsuru, Murakami Kouki, Suzuki Takashi, Tanaka Kiyoshi, Kan Toshiyuki
Department of Synthetic Organic & Medicinal Chemistry, School of Pharmaceutical Sciences, University of Shizuoka, 52-1 Yada, Suruga-ku, Shizuoka 422-8526, Japan.
Bioorg Med Chem Lett. 2007 Jun 1;17(11):3095-8. doi: 10.1016/j.bmcl.2007.03.041. Epub 2007 Mar 16.
Dideoxy-epigallocatechin gallate (DO-EGCG) (2), a simplified analog of naturally occurring EGCG (1), was efficiently prepared by directly introducing a ketone group at C3 and successive reduction to the sec-alcohol with 2,3-cis stereochemistry. Compound 2 showed potent anti-influenza virus activity, indicating that the hydroxyl substituents on the A-ring are not crucial for anti-influenza virus activity.
双脱氧表没食子儿茶素没食子酸酯（DO-EGCG）（2）是天然存在的表没食子儿茶素没食子酸酯（EGCG）（1）的简化类似物，通过直接在C3处引入酮基并随后将其还原为具有2,3-顺式立体化学的仲醇来高效制备。化合物2显示出强效的抗流感病毒活性，表明A环上的羟基取代基对于抗流感病毒活性并非至关重要。
