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Pyrrolobenzoxazepinone derivatives as non-nucleoside HIV-1 RT inhibitors: further structure-activity relationship studies and identification of more potent broad-spectrum HIV-1 RT inhibitors with antiviral activity.
Campiani G, Morelli E, Fabbrini M, Nacci V, Greco G, Novellino E, Ramunno A, Maga G, Spadari S, Caliendo G, Bergamini A, Faggioli E, Uccella I, Bolacchi F, Marini S, Coletta M, Nacca A, Caccia S. Campiani G, et al. Among authors: spadari s. J Med Chem. 1999 Oct 21;42(21):4462-70. doi: 10.1021/jm990150o. J Med Chem. 1999. PMID: 10543890
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.
Fattorusso C, Gemma S, Butini S, Huleatt P, Catalanotti B, Persico M, De Angelis M, Fiorini I, Nacci V, Ramunno A, Rodriquez M, Greco G, Novellino E, Bergamini A, Marini S, Coletta M, Maga G, Spadari S, Campiani G. Fattorusso C, et al. Among authors: spadari s. J Med Chem. 2005 Nov 17;48(23):7153-65. doi: 10.1021/jm050257d. J Med Chem. 2005. PMID: 16279773
Non-nucleoside HIV-1 reverse transcriptase inhibitors: synthesis and biological evaluation of novel quinoxalinylethylpyridylthioureas as potent antiviral agents.
Campiani G, Fabbrini M, Morelli E, Nacci V, Greco G, Novellino E, Maga G, Spadari S, Bergamini A, Faggioli E, Uccella I, Bolacchi F, Marini S, Coletta M, Fracasso C, Caccia S. Campiani G, et al. Among authors: spadari s. Antivir Chem Chemother. 2000 Mar;11(2):141-55. doi: 10.1177/095632020001100206. Antivir Chem Chemother. 2000. PMID: 10819438 Free article.
Quinoxalinylethylpyridylthioureas (QXPTs) as potent non-nucleoside HIV-1 reverse transcriptase (RT) inhibitors. Further SAR studies and identification of a novel orally bioavailable hydrazine-based antiviral agent.
Campiani G, Aiello F, Fabbrini M, Morelli E, Ramunno A, Armaroli S, Nacci V, Garofalo A, Greco G, Novellino E, Maga G, Spadari S, Bergamini A, Ventura L, Bongiovanni B, Capozzi M, Bolacchi F, Marini S, Coletta M, Guiso G, Caccia S. Campiani G, et al. Among authors: spadari s. J Med Chem. 2001 Feb 1;44(3):305-15. doi: 10.1021/jm0010365. J Med Chem. 2001. PMID: 11462972
The stereoselective targeting of a specific enzyme-substrate complex is the molecular mechanism for the synergic inhibition of HIV-1 reverse transcriptase by (R)-(-)-PPO464: a novel generation of nonnucleoside inhibitors.
Maga G, Ramunno A, Nacci V, Locatelli GA, Spadari S, Fiorini I, Baldanti F, Paolucci S, Zavattoni M, Bergamini A, Galletti B, Muck S, Hubscher U, Giorgi G, Guiso G, Caccia S, Campiani G. Maga G, et al. Among authors: spadari s. J Biol Chem. 2001 Nov 30;276(48):44653-62. doi: 10.1074/jbc.M106702200. Epub 2001 Sep 25. J Biol Chem. 2001. PMID: 11572864 Free article.
The human immunodeficiency virus type 1 (HIV-1) nonnucleoside reverse transcriptase (RT) inhibitor pyrrolopyridooxazepinone (PPO) derivative, (+/-)-PPO294, was shown to be active toward wild type and mutated HIV-1 RT and to act synergistically in combination with 3'-azido-3'-deox …
The human immunodeficiency virus type 1 (HIV-1) nonnucleoside reverse transcriptase (RT) inhibitor pyrrolopyridooxazepinone (PPO) derivative …
Effects of drug resistance mutations L100I and V106A on the binding of pyrrolobenzoxazepinone nonnucleoside inhibitors to the human immunodeficiency virus type 1 reverse transcriptase catalytic complex.
Locatelli GA, Campiani G, Cancio R, Morelli E, Ramunno A, Gemma S, Hübscher U, Spadari S, Maga G. Locatelli GA, et al. Among authors: spadari s. Antimicrob Agents Chemother. 2004 May;48(5):1570-80. doi: 10.1128/AAC.48.5.1570-1580.2004. Antimicrob Agents Chemother. 2004. PMID: 15105107 Free PMC article.
Selective targeting of the HIV-1 reverse transcriptase catalytic complex through interaction with the "primer grip" region by pyrrolobenzoxazepinone non-nucleoside inhibitors correlates with increased activity towards drug-resistant mutants.
Zanoli S, Gemma S, Butini S, Brindisi M, Joshi BP, Campiani G, Fattorusso C, Persico M, Crespan E, Cancio R, Spadari S, Hübscher U, Maga G. Zanoli S, et al. Among authors: spadari s. Biochem Pharmacol. 2008 Jul 15;76(2):156-68. doi: 10.1016/j.bcp.2008.04.009. Epub 2008 Apr 29. Biochem Pharmacol. 2008. PMID: 18541223
Potentiation of inhibition of wild-type and mutant human immunodeficiency virus type 1 reverse transcriptases by combinations of nonnucleoside inhibitors and d- and L-(beta)-dideoxynucleoside triphosphate analogs.
Maga G, Hübscher U, Pregnolato M, Ubiali D, Gosselin G, Spadari S. Maga G, et al. Among authors: spadari s. Antimicrob Agents Chemother. 2001 Apr;45(4):1192-200. doi: 10.1128/AAC.45.4.1192-1200.2001. Antimicrob Agents Chemother. 2001. PMID: 11257034 Free PMC article.
182 results