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Molecules 2016, 21(2), 221; doi:10.3390/molecules21020221

Focus on Chirality of HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors

Institute Pasteur Italy—Fondazione Cenci Bolognetti, Dipartimento di Chimica e Tecnologie del Farmaco, Sapienza Università di Roma, Piazzale Aldo Moro 5, I-00185 Roma, Italy
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Author to whom correspondence should be addressed.
Academic Editor: Derek J. McPhee
Received: 11 January 2016 / Revised: 4 February 2016 / Accepted: 8 February 2016 / Published: 16 February 2016
(This article belongs to the Special Issue Chiral Drugs)
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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. View Full-Text
Keywords: chirality; HIV-1; reverse transcriptase; non-nucleoside inhibitor chirality; HIV-1; reverse transcriptase; non-nucleoside inhibitor
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Famiglini, V.; Silvestri, R. Focus on Chirality of HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors. Molecules 2016, 21, 221.

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