顺式-5-氟-1-[2-(羟甲基)-1,3-氧硫杂环戊烷-5-基]胞嘧啶的(-)和(+)对映体的5'-三磷酸酯同样抑制人类免疫缺陷病毒1型逆转录酶。
The 5'-triphosphates of the (-) and (+) enantiomers of cis-5-fluoro-1-[2-(hydroxymethyl)-1,3-oxathiolane-5-yl]cytosine equally inhibit human immunodeficiency virus type 1 reverse transcriptase.
作者信息
Wilson J E, Martin J L, Borroto-Esoda K, Hopkins S, Painter G, Liotta D C, Furman P A
机构信息
Division of Virology, Burroughs Wellcome Co., Research Triangle Park, North Carolina 27709.
出版信息
Antimicrob Agents Chemother. 1993 Aug;37(8):1720-2. doi: 10.1128/AAC.37.8.1720.
The (-) enantiomer of cis-5-fluoro-1-[2-(hydroxymethyl)-1,3-oxathiolane-5-yl]cytosine is a potent inhibitor of human immunodeficiency virus type 1 in vitro. The 5'-triphosphates of the (-) and (+) enantiomers equally inhibited the production of full-length minus-strand DNA in an endogenous reverse transcriptase reaction, each competitively inhibited DNA synthesis, and each was used as a chain-terminating substrate.
顺式-5-氟-1-[2-(羟甲基)-1,3-氧硫杂环戊烷-5-基]胞嘧啶的(-)对映体在体外是1型人类免疫缺陷病毒的有效抑制剂。(-)和(+)对映体的5'-三磷酸酯在内源性逆转录酶反应中同等程度地抑制全长负链DNA的产生，二者均竞争性抑制DNA合成，且二者均用作链终止底物。
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