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Synthesis of nucleotide analogues, EFdA, EdA and EdAP, and the effect of EdAP on hepatitis B virus replication.
Bioscience, Biotechnology, and Biochemistry ( IF 1.4 ) Pub Date : 2019-10-07 , DOI: 10.1080/09168451.2019.1673696
Mai Kamata 1 , Toshifumi Takeuchi 1 , Ei Hayashi 1 , Kazane Nishioka 1, 2 , Mizuki Oshima 1, 2 , Masashi Iwamoto 1, 2 , Kota Nishiuchi 1 , Shogo Kamo 1 , Shusuke Tomoshige 1 , Koichi Watashi 1, 2 , Shinji Kamisuki 3 , Hiroshi Ohrui 4 , Fumio Sugawara 1 , Kouji Kuramochi 1
Affiliation  

4'-Ethynyl-2-fluoro-2'-deoxyadenosine (EFdA) and 4'-ethynyl-2'-deoxyadenosine (EdA) are nucleoside analogues which inhibit human immunodeficiency virus type 1 (HIV-1) reverse transcriptase. EdAP, a cyclosaligenyl (cycloSal) phosphate derivative of EdA, inhibits the replication of the influenza A virus. The common structural feature of these compounds is the ethynyl group at the 4'-position. In this study, these nucleoside analogues were prepared by a common synthetic strategy starting from the known 1,2-di-O-acetyl-D-ribofuranose. Biological evaluation of EdAP revealed that this compound reduced hepatitis B virus (HBV) replication dose-dependently without cytotoxicity against host cells tested in this study.

中文翻译:

核苷酸类似物EFdA,EdA和EdAP的合成,以及EdAP对乙型肝炎病毒复制的影响。

4′-乙炔基-2-氟-2′-脱氧腺苷(EFdA)和4′-乙炔基-2′-脱氧腺苷(EdA)是抑制人免疫缺陷病毒1型(HIV-1)逆转录酶的核苷类似物。EdAP,EdA的磷酸环saligenyl(cycloSal)衍生物,可抑制甲型流感病毒的复制。这些化合物的共同结构特征是在4'-位的乙炔基。在这项研究中,这些核苷类似物是通过一种常见的合成策略从已知的1,2-二-O-乙酰基-D-呋喃核糖开始制备的。EdAP的生物学评估表明,该化合物可剂量依赖性地减少乙型肝炎病毒(HBV)复制,而对本研究中测试的宿主细胞无细胞毒性。
更新日期:2019-12-19
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