Specific targeting highly conserved residues in the HIV-1 reverse transcriptase primer grip region. Design, synthesis, and biological evaluation of novel, potent, and broad spectrum NNRTIs with antiviral activity.

doi:10.1021/jm050257d

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Article

Specific targeting highly conserved residues in the HIV-1 reverse transcriptase primer grip region. Design, synthesis, and biological evaluation of novel, potent, and broad spectrum NNRTIs with antiviral activity.

Journal of medicinal chemistry - 17 Nov 2005

Fattorusso Caterina, Gemma Sandra, Butini Stefania, Huleatt Paul, Catalanotti Bruno, Persico Marco, De Angelis Meri, Fiorini Isabella, Nacci Vito, Ramunno Anna, Rodriquez Manuela, Greco Giovanni, Novellino Ettore, Bergamini Alberto, Marini Stefano, Coletta Massimo, Maga Giovanni, Spadari Silvio, Campiani Giuseppe

Abstract excerpt

Pyrrolobenzoxazepinones (PBOs) represent a new class of human immunodeficiency virus type 1 (HIV-1) nonnucleoside reverse transcriptase (RT) inhibitors (NNRTIs) whose prototype is 5. Molecular modeling studies based on the X-ray structures of HIV-1 RT prompted the synthesis of novel analogues which were tested as anti-HIV agents. The PBO derivatives specifically designed to target the highly conserved amino acid...

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PMID: 16279773
DOI: 10.1021/jm050257d

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