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Synthesis of the 5-phosphono-pent-2-en-1-yl nucleosides: A new class of antiviral acyclic nucleoside phosphonates

机译:5-膦酰基-戊-2-烯-1-基核苷的合成:一类新的抗病毒无环核苷膦酸酯

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摘要

A new class of acyclic nucleoside phosphonates, the 5-phosphono-pent-2-en-1-yl nucleosides and their hexadecyloxypro-pyl esters, were synthesized from butyn-1-ol. Only the hexadecyloxypropyl esters showed antiviral activity against herpes simplex virus type 1, in vitro. Hexadecyloxypropyl 1-(5-phosphono-pent-2-en-1-yl)-thymine was the most active and selective compound among the synthesized nucleotides with an EC_(50) value of 0.90 μM.
机译:由丁炔-1-醇合成了一类新型的无环核苷膦酸酯,即5-膦酰基-戊-2-烯-1-基核苷及其十六烷基氧基丙基酯。在体外,仅十六烷氧基丙基酯显示出对1型单纯疱疹病毒的抗病毒活性。十六烷基氧丙基1-(5-膦酰基-戊-2-烯-1-基)-胸腺嘧啶是合成核苷酸中最具活性和选择性的化合物,EC_(50)值为0.90μM。

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