Abstract
Chiral HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) are of great interest since one enantiomer is often more potent than the corresponding counterpart against the HIV-1 wild type (WT) and the HIV-1 drug resistant mutant strains. This review exemplifies the various studies made to investigate the effect of chirality on the antiretroviral activity of top HIV-1 NNRTI compounds, such as nevirapine (NVP), efavirenz (EFV), alkynyl- and alkenylquinazolinone DuPont compounds (DPC), diarylpyrimidine (DAPY), dihydroalkyloxybenzyloxopyrimidine (DABO), phenethylthiazolylthiourea (PETT), indolylarylsulfone (IAS), arylphosphoindole (API) and trifluoromethylated indole (TFMI) The chiral separation, the enantiosynthesis, along with the biological properties of these HIV-1 NNRTIs, are discussed.
Highlights
Human immunodeficiency virus type 1 (HIV-1) is the etiological agent of acquired immune deficiency syndrome (AIDS), a global pandemic disease which has claimed the lives of more than 34 million people so far
The treatment of HIV infected people is based on antiretroviral therapy (ART), known as highly active antiretroviral therapy (HAART), which combines three or more drugs that suppress HIV replication [1]
The ART regimens for a treatment-naive patient combines three or more antiretroviral drugs, generally two nucleoside reverse transcriptase inhibitors with a third non-nucleoside antiretroviral drug: a reverse transcriptase inhibitor, a protease inhibitor or an integrase strand transfer inhibitor [28]
Summary
Human immunodeficiency virus type 1 (HIV-1) is the etiological agent of acquired immune deficiency syndrome (AIDS), a global pandemic disease which has claimed the lives of more than 34 million people so far. The treatment of HIV infected people is based on antiretroviral therapy (ART), known as highly active antiretroviral therapy (HAART), which combines three or more drugs that suppress HIV replication [1]. NNRTIs of HIV-1 are key drugs for the treatment of AIDS [16,17,18]. Thanks to their specificity for HIV-1, which makes them very selective inhibitors, NNRTIs became standard components of ART regimens [19,20]. The ART regimens for a treatment-naive patient combines three or more antiretroviral drugs, generally two nucleoside reverse transcriptase inhibitors with a third non-nucleoside antiretroviral drug: a reverse transcriptase inhibitor, a protease inhibitor or an integrase strand transfer inhibitor [28]. We focused on the chemical modification of chiral atoms that to our knowledge was not exhaustively reviewed
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