Synthesis of 3′-halo-5′-norcarbocyclic nucleoside phosphonates as potent anti-HIV agents
作者:Nadège Hamon、Malika Kaci、Jean-Pierre Uttaro、Christian Périgaud、Christophe Mathé
DOI:10.1016/j.ejmech.2018.03.038
日期:2018.4
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.
描述了3'-卤代(碘和氟)5'-降碳环核苷膦酸酯的合成和抗病毒评价。没有观察到针对寨卡病毒,登革热病毒2,HSV-1,HSV-2和基孔肯雅病毒的抗病毒活性。相反,某些合成的化合物是有效的HIV-1复制抑制剂,与(R)-PMPA相比,没有伴随的细胞毒性。