4.5 Review

Recent Advances in the Design and Development of Non-nucleoside Reverse Transcriptase Inhibitor Scaffolds

Journal

CHEMMEDCHEM
Volume 14, Issue 1, Pages 52-77

Publisher

WILEY-V C H VERLAG GMBH
DOI: 10.1002/cmdc.201800577

Keywords

antiviral; drug design; inhibitors; molecular hybridization; reverse transcriptase

Funding

  1. Isfahan University of Medical Science

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Non-nucleoside reverse transcriptase inhibitors (NNRTIs) have always been an important part of the anti-HIV-1 combination therapy known as combination antiretroviral therapy (cART) since 1996. The use of NNRTIs for about 22 years has led to some mutations in the residues that compose the reverse transcriptase active site, resulting in the emergence of drug-resistant viruses. Thus, the search for new potent NNRTIs with an improved safety profile and activity against drug-resistant HIV strains is indispensable, and many hit and lead NNRTIs have been discovered in the last decade. This review provides an overview of the development in this field from 2013 to August 2018.

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