一种高活性新型抗艾滋病毒药物2',3'-二脱氢-3'-脱氧-4'-乙炔基胸腺嘧啶的合成。
Synthesis of a highly active new anti-HIV agent 2',3'-didehydro-3'-deoxy-4'-ethynylthymidine.
作者信息
Haraguchi Kazuhiro, Takeda Shingo, Tanaka Hiromichi, Nitanda Takao, Baba Masanori, Dutschman G E, Cheng Yung-Chi
机构信息
School of Pharmaceutical Sciences, Showa University, 1-5-8 Hatanodai, Shinagawa-ku, Tokyo 142-8555, Japan.
出版信息
Bioorg Med Chem Lett. 2003 Nov 3;13(21):3775-7. doi: 10.1016/j.bmcl.2003.07.009.
Compounds having methyl, vinyl, and ethynyl groups at the 4'-position of stavudine (d4T: 2',3'-didehydro-3'-deoxythymidine) were synthesized. The compounds were assayed for their ability to inhibit the replication of HIV in cell culture. The 4'-ethynyl analogue (15) was found to be more potent and less toxic than the parent compound stavudine.
合成了在司他夫定（d4T：2'，3'-二脱氢-3'-脱氧胸苷）的4'-位具有甲基、乙烯基和乙炔基的化合物。测定了这些化合物在细胞培养物中抑制HIV复制的能力。发现4'-乙炔基类似物（15）比母体化合物司他夫定更有效且毒性更小。
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