Abstract
Along with nucleoside reverse transcriptase inhibitors (NRTIs) and protease inhibitors (PIs), nonnucleoside reverse transcriptase inhibitors (NNRTIs) have gained a definitive and important place in the treatment of HIV-1 infections, and are in rapid development. These compounds can be grouped into two classes: the first generation NNRTIs, mainly discovered by random screening, and the second generation NNRTIs, developed as a result of comprehensive strategies involving molecular modelling, rationale-based drug synthesis, biological and pharmacokinetic evaluations. The recent boom of NNRTIs is mainly due to their antiviral potency, high specificity and low toxicity. The rapid emergence of drug-resistant HIV-1 strains induced by the first generation drugs is a disadvantage bypassed, in part, by the broad spectrum second generation NNRTIs. Starting from the first generation, this review will focus on the second generation NNRTIs dealing with the recent and most interesting published results, highlighting the guidelines for the development of a third generation of NNRTIs.
Keywords: Non-nucleoside hiv-1 reverse transcriptase (rt) inhibitors, Nucleoside reverse transcriptase inhibitors(nrtis), Protease inhibitors(pls), hept, Tsao-t, Tsao-t analogues, Dabo antiviral agents, Dihydroalkoxybenzyloxypyrimidines(dabo), Benzodiazepinones(tibo)
Current Pharmaceutical Design
Title: Non-Nucleoside HIV-1 Reverse Transcriptase (RT) Inhibitors: Past, Present, and Future Perspectives
Volume: 8 Issue: 8
Author(s): Giuseppe Campiani, Anna Ramunno, Giovanni Maga, Vito Nacci, Caterina Fattorusso, Bruno Catalanotti, Elena Morelli and Ettore Novellino
Affiliation:
Keywords: Non-nucleoside hiv-1 reverse transcriptase (rt) inhibitors, Nucleoside reverse transcriptase inhibitors(nrtis), Protease inhibitors(pls), hept, Tsao-t, Tsao-t analogues, Dabo antiviral agents, Dihydroalkoxybenzyloxypyrimidines(dabo), Benzodiazepinones(tibo)
Abstract: Along with nucleoside reverse transcriptase inhibitors (NRTIs) and protease inhibitors (PIs), nonnucleoside reverse transcriptase inhibitors (NNRTIs) have gained a definitive and important place in the treatment of HIV-1 infections, and are in rapid development. These compounds can be grouped into two classes: the first generation NNRTIs, mainly discovered by random screening, and the second generation NNRTIs, developed as a result of comprehensive strategies involving molecular modelling, rationale-based drug synthesis, biological and pharmacokinetic evaluations. The recent boom of NNRTIs is mainly due to their antiviral potency, high specificity and low toxicity. The rapid emergence of drug-resistant HIV-1 strains induced by the first generation drugs is a disadvantage bypassed, in part, by the broad spectrum second generation NNRTIs. Starting from the first generation, this review will focus on the second generation NNRTIs dealing with the recent and most interesting published results, highlighting the guidelines for the development of a third generation of NNRTIs.
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Cite this article as:
Campiani Giuseppe, Ramunno Anna, Maga Giovanni, Nacci Vito, Fattorusso Caterina, Catalanotti Bruno, Morelli Elena and Novellino Ettore, Non-Nucleoside HIV-1 Reverse Transcriptase (RT) Inhibitors: Past, Present, and Future Perspectives, Current Pharmaceutical Design 2002; 8 (8) . https://dx.doi.org/10.2174/1381612024607207
DOI https://dx.doi.org/10.2174/1381612024607207 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
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