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1 2003

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Inhibitory integrazy HIV

Niedbała H., Polański J., Gieleciak R.

Wiadomości Chemiczne

2003

[Z] 57, 3-4

289--303

AZT was a first anti-HIV drug found during screening performed by National Institute of Health (Bethesda, USA). Anti-HIV drugs or potential drugs grouped according to the molecular target or compound class can be found in the NIH database at [http://www.niaid.nih.gov/daids/dtpdb/intro.htm]. HIV integrase is one of the potential targets of anti-HIV drugs. Integrase is an enzyme that catalyzes the insertion of retrotranscribed viral DNA into the cellular host genome. Its structure is known but until now there is no certified drug targeted at this enzyme. In the 90' several integrase inhibitors were described. The investigations of these compounds allowed finding new active compounds, e.g., styrylchinolines that was described in recent years. In particular, the current publication discusses structure-activity relationships (SAR) for these compounds. It appeared that the SAR data from ex-vivo experiments can be both visualized and interpreted by the use of the Kohonen maps of the electrostatic potetntial of the molecular surface as shown in Figure 2. Finally, the results of the Merck investigations on HIV-1 integrase inhibitors have been briefly discussed.