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N-取代的3'-氨基-3'-脱氧胸苷的合成及其抗HIV的生物学评价。

Synthesis of N-substituted 3'-amino-3'-deoxythymidines and their biological evaluation against HIV.

作者信息

Motawia M S, Pedersen E B, Nielsen C M

机构信息

Department of Chemistry, Odense University, Denmark.

出版信息

Arch Pharm (Weinheim). 1990 Dec;323(12):971-5. doi: 10.1002/ardp.19903231207.

DOI:10.1002/ardp.19903231207
PMID:2096799
Abstract

Treatment of 3'-amino-3'-deoxythymidine (1) with carboxylic acid anhydrides afforded the corresponding acylamino derivatives 2a-f. Reaction of 1 with a variety of isothiocyanates led to the corresponding thioureido derivatives 3a-i. Also, conversion of 1 into 3'-carbylamino-3'-deoxythymidine (7) is reported. The compounds 2, 3, and 8 were evaluated for their anti-HIV activity in MT-4 cells, but did not show sufficient efficacy.

摘要

用羧酸酐处理3'-氨基-3'-脱氧胸苷（1）得到相应的酰氨基衍生物2a-f。1与各种异硫氰酸酯反应生成相应的硫脲基衍生物3a-i。此外，还报道了将1转化为3'-氨基甲酰基-3'-脱氧胸苷（7）的过程。对化合物2、3和8在MT-4细胞中进行了抗HIV活性评估，但未显示出足够的疗效。

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