http://www.cnr.it/ontology/cnr/individuo/prodotto/ID27553
Specific Targeting of Highly Conserved Residues in the HIV-1 Reverse Transcriptase Primer Grip Region. 2. Stereoselective Interaction to Overcome the Effects of Drug Resistant Mutations. (Articolo in rivista)
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- Specific Targeting of Highly Conserved Residues in the HIV-1 Reverse Transcriptase Primer Grip Region. 2. Stereoselective Interaction to Overcome the Effects of Drug Resistant Mutations. (Articolo in rivista) (literal)
- Anno
- 2009-01-01T00:00:00+01:00 (literal)
- Alternative label
Butini S, Brindisi M, Cosconati S, Marinelli L, Borrelli G, Coccone SS, Ramunno A, Campiani G, Novellino E, Zanoli S, Samuele A, Giorgi G, Bergamini A, Mattia MD, Lalli S, Galletti B, Gemma S, Maga G. (2009)
Specific Targeting of Highly Conserved Residues in the HIV-1 Reverse Transcriptase Primer Grip Region. 2. Stereoselective Interaction to Overcome the Effects of Drug Resistant Mutations.
in Journal of medicinal chemistry
(literal)
- Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#autori
- Butini S, Brindisi M, Cosconati S, Marinelli L, Borrelli G, Coccone SS, Ramunno A, Campiani G, Novellino E, Zanoli S, Samuele A, Giorgi G, Bergamini A, Mattia MD, Lalli S, Galletti B, Gemma S, Maga G. (literal)
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- ISI Web of Science (WOS) (literal)
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- European Research Centre for Drug Discovery and Development (NatSynDrugs), Universita di Siena, Italy, Dipartimento Farmaco Chimico Tecnologico (DFCT), Universita di Siena, via Aldo Moro 2, 53100 Siena, Italy, Dipartimento di Chimica Farmaceutica e Tossicologica (DCF&T), Universita di Napoli Federico II, via D. Montesano 49, 80131 Napoli, Italy, Istituto di Genetica Molecolare (IGM)CNR, via Abbiategrasso 207, 27100 Pavia, Italy, Dipartimento di Chimica (DC), Universita di Siena, via Aldo Moro 2, 53100 Siena, Italy, Dipartimento di Sanita Pubblica e Biologia Cellulare, Universita degli Studi di Roma \"Tor Vergata\", via Tor Vergata 135, 00133 Roma, Italy, Sigma-Tau Industrie Farmaceutiche Riunite spa, Via Pontina Km 30,400, 00040 Pomezia, Italy. (literal)
- Titolo
- Specific Targeting of Highly Conserved Residues in the HIV-1 Reverse Transcriptase Primer Grip Region. 2. Stereoselective Interaction to Overcome the Effects of Drug Resistant Mutations. (literal)
- Abstract
- Starting from the prototypic compound 4, we describe new, potent, and broad-spectrum pyrrolobenzo(pyrido)oxazepinones antivirals. A biochemical and enzymological investigation was performed for defining their mechanism of inhibition at either recombinant HIV-1 RT wild type and non-nucleoside reverse transcriptase inhibitors (NNRTIs)-resistant mutants. For the novel compounds (S)-(+)-5 and (S)-(-)-7, a clear-cut stereoselective mechanism of enzyme inhibition was found. Molecular modeling studies were performed for revealing the underpinnings of this behavior. (literal)
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