Potential drugs for the treatment of AIDS.
From our investigations the following compounds have emerged as particularly potent and selective inhibitors of HIV replication: sulphated polysaccharides (i.e. heparin, dextran sulphate, pentosan polysulphate), dideoxynucleoside analogues such as the 3'-azido-and 3'-fluoro-substituted 2',3'-dideoxyribosides of both purines (i.e. guanine, 2,6-diaminopurine) and pyrimidines (i.e. uracil, thymine), and the 9-(2-phosphonylmethoxyethyl) derivatives of adenine, 2-monoaminopurine and 2,6-diaminopurine. All these compounds yield great promise for the treatment of retrovirus infections in humans. Whereas the sulphated polysaccharides interfere with the virus adsorption process, the nucleoside analogues (following intracellular phosphorylation to their 5'-triphosphate) appear to be targeted at the reverse transcriptase.
De Clercq
E
E
Rega Institute for Medical Research, Katholieke Universiteit Leuven, Belgium.
D000163:Acquired Immunodeficiency Syndrome / Q000188:drug therapy*; D006678:HIV / Q000187:drug effects* / Q000502:physiology; D006801:Humans; D014779:Virus Replication / Q000187:drug effects