Combinatorial Chemistry as a Tool for Targeting Different Stages of the Replicative HIV-1 Cycle

Title: Combinatorial Chemistry as a Tool for Targeting Different Stages of the Replicative HIV-1 Cycle

Volume: 8 Issue: 5

Author(s): Claudia Mugnaini, Elena Petricci, Federico Corelli and Maurizio Botta

Affiliation:

Keywords: hiv, libraries, antiretroviral drugs, reverse transcriptase inhibitors, protease inhibitors, integrase inhibitors, entry inhibitors, tat and rev inhibitors

Abstract: In the present era, acquired immunodeficiency syndrome (AIDS) is the most fatal disorder for which no completely successful chemotherapy has been developed so far. The pandemic spread of this disease has prompted an unprecedented scientific and clinical effort to understand and combat it. A number of targets has been identified to stop the replication of the virus at different stages of its life cycle: Reverse Transcriptase (RT), protease (PR) and CCR5 are the most promising targets. Although highly active antiretroviral therapy (HAART) has been effective in reducing the mortality and morbidity in recent years, adverse side effects of the chemotherapy, patient non-compliance and the development of viral resistance remain major problems. With the aim to find better drug candidates with minor adverse side effects in recent years, several groups have investigated combinatorial approaches for the generation of libraries of HIV PR inhibitors while only few contributions to the preparation of libraries of HIV Reverse Transcriptase (RT) and CCR5 inhibitors are available. This review summarizes the recent developments of combinatorial chemistry in this area.

Cite this article as:

Mugnaini Claudia, Petricci Elena, Corelli Federico and Botta Maurizio, Combinatorial Chemistry as a Tool for Targeting Different Stages of the Replicative HIV-1 Cycle, Combinatorial Chemistry & High Throughput Screening 2005; 8 (5) . https://dx.doi.org/10.2174/1386207054546504