不同三苯甲基化嘧啶和嘌呤核苷类似物的抗黄病毒活性
Anti-flavivirus Activity of Different Tritylated Pyrimidine and Purine Nucleoside Analogues.
作者信息
McGuigan Christopher, Serpi Michaela, Slusarczyk Magdalena, Ferrari Valentina, Pertusati Fabrizio, Meneghesso Silvia, Derudas Marco, Farleigh Laura, Zanetta Paola, Bugert Joachim
机构信息
School of Pharmacy and Pharmaceutical Sciences Cardiff University King Edward VII Avenue Cardiff CF10 3NB United Kingdom.
Medical Microbiology and Infectious Diseases School of Medicine Cardiff University Heath Park Cardiff CF14 4XN United Kingdom.
出版信息
ChemistryOpen. 2016 Jan 21;5(3):227-35. doi: 10.1002/open.201500216. eCollection 2016 Jun.
A series of tritylated and dimethoxytritylated analogues of selected pyrimidine and purine nucleosides were synthesized and evaluated for their in vitro inhibitory activity against two important members of the genus Flavivirus in the Flaviviridae family, the yellow fever (YFV) and dengue viruses (DENV). Among all compounds tested, the 5'-O-tritylated and the 5'-O-dimethoxytritylated 5-fluorouridine derivatives exerted potency against YFV. Interestingly in the series of purine analogues, the 5'O, N-bis-tritylated fludarabine derivative revealed strong inhibitory activity against DENV at μm concentrations, however significantly weaker potency against YFV.
合成了一系列选定嘧啶和嘌呤核苷的三苯甲基化和二甲氧基三苯甲基化类似物，并评估了它们对黄病毒科黄病毒属的两个重要成员黄热病毒（YFV）和登革病毒（DENV）的体外抑制活性。在所有测试的化合物中，5'-O-三苯甲基化和5'-O-二甲氧基三苯甲基化的5-氟尿苷衍生物对YFV具有效力。有趣的是，在嘌呤类似物系列中，5'O，N-双三苯甲基化的氟达拉滨衍生物在微摩尔浓度下对DENV显示出强抑制活性，但对YFV的效力明显较弱。
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