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作为强效抗艾滋病毒药物的3'-卤代-5'-去碳环核苷膦酸酯的合成。

Synthesis of 3'-halo-5'-norcarbocyclic nucleoside phosphonates as potent anti-HIV agents.

作者信息

Hamon Nadège, Kaci Malika, Uttaro Jean-Pierre, Périgaud Christian, Mathé Christophe

机构信息

Institut des Biomolécules Max Mousseron (IBMM), UMR 5247, Université de Montpellier, CNRS, ENSCM, cc 1705, Site Triolet, Place Eugène Bataillon, 34095, Montpellier cedex 5, France.

Institut des Biomolécules Max Mousseron (IBMM), UMR 5247, Université de Montpellier, CNRS, ENSCM, cc 1705, Site Triolet, Place Eugène Bataillon, 34095, Montpellier cedex 5, France.

出版信息

Eur J Med Chem. 2018 Apr 25;150:642-654. doi: 10.1016/j.ejmech.2018.03.038. Epub 2018 Mar 14.

DOI:10.1016/j.ejmech.2018.03.038
PMID:29558735
Abstract

The synthesis and the antiviral evaluation of 3'-halo (iodo and fluoro) 5'-norcarbocyclic nucleoside phosphonates is described. No antiviral activity was observed against Zika virus, Dengue virus 2, HSV-1, HSV-2 and Chikungunya virus. In contrast, some of the synthesized compounds are potent inhibitors of the replication of HIV-1, comparatively to (R)-PMPA, with no concomitant cytotoxicity.

摘要

本文描述了3'-卤代（碘代和氟代）5'-降碳环核苷膦酸酯的合成及其抗病毒活性评估。未观察到其对寨卡病毒、登革热病毒2型、单纯疱疹病毒1型、单纯疱疹病毒2型和基孔肯雅病毒具有抗病毒活性。相比之下，与（R）-替诺福韦酯相比，一些合成化合物是HIV-1复制的有效抑制剂，且无伴随的细胞毒性。

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