Novel L-lyxo and 5'-deoxy-5'-modified TSAO-T analogs: Synthesis and anti-HIV-1 activity

被引：6

作者：

Ingate, S

DeClercq, E

Balzarini, J

Camarasa, MJ

机构：

[1] CSIC, INST QUIM MED, E-28006 MADRID, SPAIN

[2] CATHOLIC UNIV LEUVEN, REGA INST MED RES, B-3000 LOUVAIN, BELGIUM

来源：

ANTIVIRAL RESEARCH | 1996年 / 32卷 / 03期

关键词：

HIV; HIV-1-specific reverse transcriptase inhibitor; TSAO-T; L-lyxo-TSAO-T; 5'-deoxy-5'-modified TSAO-T; 3'-spironucleoside; reverse transcriptase inhibitor; AIDS;

D O I：

10.1016/S0166-3542(95)00989-2

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

Novel L-lyxo-TSAO-T analogs with an inverted configuration at the C-4'-position of the sugar moiety and 5'-deoxy-5'-modified TSAO-T derivatives have been prepared and evaluated for their inhibitory effect on human immunodeficiency virus type 1 (HIV-1) and type 2 (HIV-2) replication in cell culture. None of the compounds showed marked antiviral efficacy. The inactivity of the TSAO-T derivatives may most likely be explained by either their different 4'-configuration or their different chemical structure that may not allow an optimal interaction of the molecules with the lipophilic binding pocket of the HIV-1 reverse transcriptase.

引用

页码：149 / 164

页数：16

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