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膦酸化碳环2'-氧杂-3'-氮杂核苷作为新型抗逆转录病毒药物。

Phosphonated carbocyclic 2'-oxa-3'-azanucleosides as new antiretroviral agents.

作者信息

Chiacchio Ugo, Rescifina Antonio, Iannazzo Daniela, Piperno Anna, Romeo Roberto, Borrello Luisa, Sciortino Maria Teresa, Balestrieri Emanuela, Macchi Beatrice, Mastino Antonio, Romeo Giovanni

机构信息

Dipartimento di Scienze Chimiche, Università di Catania, Viale Andrea Doria 6, Catania 95125, Italy.

出版信息

J Med Chem. 2007 Jul 26;50(15):3747-50. doi: 10.1021/jm070285r. Epub 2007 Jun 20.

Abstract

Phosphonated carbocyclic 2'-oxa-3'-azanucleosides have been synthesized and tested for their antiretroviral activity. The obtained results have shown that some of the compounds were as powerful as azydothymidine in inhibiting the reverse transcriptase activity of the human retrovirus T-cell leukemia/lymphotropic virus type 1 and in protecting human peripheral blood mononuclear cells against human retrovirus T-cell leukemia/lymphotropic virus type 1 transmission in vitro. These data indicate that phosphonated carbocyclic 2'-oxa-3'-azanucleosides possess the necessary requirements to efficiently counteract infections caused by human retroviruses.

摘要

膦酸化碳环2'-氧杂-3'-氮杂核苷已被合成并测试其抗逆转录病毒活性。所得结果表明,一些化合物在抑制人类逆转录病毒T细胞白血病/1型嗜淋巴细胞病毒的逆转录酶活性以及在体外保护人类外周血单核细胞免受人类逆转录病毒T细胞白血病/1型嗜淋巴细胞病毒感染方面与齐多夫定一样有效。这些数据表明,膦酸化碳环2'-氧杂-3'-氮杂核苷具备有效对抗人类逆转录病毒感染的必要条件。

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