Authors: Campiani, G.; Ramunno, A.; Maga, G.; Nacci, V.; Fattorusso, C.; Catalanotti, B.; Morelli, E.; Novellino, E.

Source: Current Pharmaceutical Design, Volume 8, Number 8, 1 April 2002 , pp. 615-657(43)

Publisher: Bentham Science Publishers

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) in; Nucleoside reverse transcriptase inhibitors(nrtis); Protease inhibitors(pls); hept; Tsao-t; Tsao-t analogues; Dabo antiviral agents; Dihydroalkoxybenzyloxypyrimidines(dabo); Benzodiazepinones(tibo)

Document Type: Review article

DOI: http://dx.doi.org/10.2174/1381612024607207

Publication date: 2002-04-01

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• Current Pharmaceutical Design publishes timely in-depth reviews covering all aspects of current research in rational drug design. Each issue is devoted to a single major therapeutic area. A Guest Editor who is an acknowledged authority in a therapeutic field has solicits for each issue comprehensive and timely reviews from leading researchers in the pharmaceutical industry and academia.
  
  Each thematic issue of Current Pharmaceutical Design covers all subject areas of major importance to modern drug design, including: medicinal chemistry, pharmacology, drug targets and disease mechanism.

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