140(P-96) 多剤耐性HIVに有効なヌクレオシドの創製(ポスター発表の部)

概要

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4'-C-Ethynyl-β-D-arabino- and 4'-C-ethyny1-2'-deoxy-β-D-ribo-pentofuranosyl pyrimidine and purine nucleosides were synthesized, and evaluated for their in vitro anti-HIV activity. The key intermediate, 4-C-ethynyl or 4-C-triethylsilylethynyl-α-D-ribo-pentofuranose, was prepared from D-glucose and glycosidated with various pyrimidine or purine bases. The arabino pyrimidine derivatives were prepared from the corresponding ribo derivatives via O^2-2'-cyclonucleosides. The 2'-deoxyribo derivatives were synthesized by radical reduction of 2'-bromo or 2'-phenoxythio-carbonyloxy nucleosides. These 4'-C-ethynyl nucleosides were proved to be potent against HIV-1 in vitro with EC_<50> values ranging 0.0003 to 0.61μM. These compounds also exerted an activity against multi-dideoxynucleoside-resistant HIV-1 strains with comparable EC_<50> values.
天然有機化合物討論会の論文
2000-10-01