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首页> 外文期刊>Zeitschrift fur Naturforschung, B. A Journal of Chemical Sciences >Synthesis and Modeling Study of Some Potential Pyrimidine Derivatives as HIV Inhibitors
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Synthesis and Modeling Study of Some Potential Pyrimidine Derivatives as HIV Inhibitors

机译：某些潜在的嘧啶衍生物作为HIV抑制剂的合成和建模研究

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摘要

A new series of 2-amino-6-((4-aryldiazenyl)benzyloxy)-4-chloropyrimidine derivatives 4 - 13 and 2,6-diamino-5-arylazo-4-chloro-pyrimidine analogs 15 - 20 were synthesized from the pyrimidine scaffolds 3 and 14, respectively, via diazotization with various amines. Nucleophilic displacement at the 2,4-diamino-5-arylazo-6-chloro-pyrimidine 16 by different amines afforded the 4-alkylamino analogs 21 - 27. All new compounds were evaluated for their in vitro anti-HIV activity in MT-4 cells as non-nucleoside reverse transcriptase inhibitors on the basis of our previous work. Screening results indicated that 10 and 11 were found to be the only compounds in the series inhibiting HIV-1 replication in cell cultures with EC_(50) of >1:23 and >2:92 μg mL~(-1) of a CC_(50) of 12.30 and 17.52 μg mL~(-1), resulting in a selectivity index of 10 and 6, respectively. In addition, preliminary structure-activity relationships and molecular modeling of these new analogs are detailed in this manuscript.
机译：合成了一系列新的2-氨基-6-（（（4-芳基二氮烯基）苄氧基）-4-氯嘧啶衍生物4-13和2,6-二氨基-5-芳基偶氮-4-氯嘧啶类似物15-20。嘧啶支架3和14分别通过各种胺进行重氮化。通过不同的胺在2,4-二氨基-5-芳基偶氮-6-氯嘧啶上的亲核取代提供了4-烷基氨基类似物21-27。评估了所有新化合物在MT-4中的体外抗HIV活性细胞作为非核苷类逆转录酶抑制剂的基础。筛选结果表明，在EC_（50）> 1:23和> 2:92μgmL〜（-1）CC_的细胞培养物中，发现10和11是唯一抑制HIV-1复制的化合物。 （50）为12.30和17.52μgmL〜（-1），选择性指数分别为10和6。另外，这些新类似物的初步构效关系和分子模型在本手稿中进行了详细介绍。

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