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Discovery and synthesis of HIV integrase inhibitors: development of potent and orally bioavailable N-methyl pyrimidones.
Gardelli C, Nizi E, Muraglia E, Crescenzi B, Ferrara M, Orvieto F, Pace P, Pescatore G, Poma M, Ferreira Mdel R, Scarpelli R, Homnick CF, Ikemoto N, Alfieri A, Verdirame M, Bonelli F, Paz OG, Taliani M, Monteagudo E, Pesci S, Laufer R, Felock P, Stillmock KA, Hazuda D, Rowley M, Summa V. Gardelli C, et al. J Med Chem. 2007 Oct 4;50(20):4953-75. doi: 10.1021/jm0704705. Epub 2007 Sep 8. J Med Chem. 2007. PMID: 17824681
Dihydroxypyrimidine-4-carboxamides as novel potent and selective HIV integrase inhibitors.
Pace P, Di Francesco ME, Gardelli C, Harper S, Muraglia E, Nizi E, Orvieto F, Petrocchi A, Poma M, Rowley M, Scarpelli R, Laufer R, Gonzalez Paz O, Monteagudo E, Bonelli F, Hazuda D, Stillmock KA, Summa V. Pace P, et al. Among authors: gardelli c. J Med Chem. 2007 May 3;50(9):2225-39. doi: 10.1021/jm070027u. Epub 2007 Apr 12. J Med Chem. 2007. PMID: 17428043
Design and synthesis of bicyclic pyrimidinones as potent and orally bioavailable HIV-1 integrase inhibitors.
Muraglia E, Kinzel O, Gardelli C, Crescenzi B, Donghi M, Ferrara M, Nizi E, Orvieto F, Pescatore G, Laufer R, Gonzalez-Paz O, Di Marco A, Fiore F, Monteagudo E, Fonsi M, Felock PJ, Rowley M, Summa V. Muraglia E, et al. Among authors: gardelli c. J Med Chem. 2008 Feb 28;51(4):861-74. doi: 10.1021/jm701164t. Epub 2008 Jan 25. J Med Chem. 2008. PMID: 18217703
Discovery of raltegravir, a potent, selective orally bioavailable HIV-integrase inhibitor for the treatment of HIV-AIDS infection.
Summa V, Petrocchi A, Bonelli F, Crescenzi B, Donghi M, Ferrara M, Fiore F, Gardelli C, Gonzalez Paz O, Hazuda DJ, Jones P, Kinzel O, Laufer R, Monteagudo E, Muraglia E, Nizi E, Orvieto F, Pace P, Pescatore G, Scarpelli R, Stillmock K, Witmer MV, Rowley M. Summa V, et al. Among authors: gardelli c. J Med Chem. 2008 Sep 25;51(18):5843-55. doi: 10.1021/jm800245z. J Med Chem. 2008. PMID: 18763751
Inhibitors of the hepatitis C virus NS3 protease with basic amine functionality at the P3-amino acid N-terminus: discovery and optimization of a new series of P2-P4 macrocycles.
Harper S, Ferrara M, Crescenzi B, Pompei M, Palumbi MC, DiMuzio JM, Donghi M, Fiore F, Koch U, Liverton NJ, Pesci S, Petrocchi A, Rowley M, Summa V, Gardelli C. Harper S, et al. Among authors: gardelli c. J Med Chem. 2009 Aug 13;52(15):4820-37. doi: 10.1021/jm900372w. J Med Chem. 2009. PMID: 19624135
Capped dipeptide phenethylamide inhibitors of the HCV NS3 protease.
Nizi E, Koch U, Ontoria JM, Marchetti A, Narjes F, Malancona S, Matassa VG, Gardelli C. Nizi E, et al. Among authors: gardelli c. Bioorg Med Chem Lett. 2004 May 3;14(9):2151-4. doi: 10.1016/j.bmcl.2004.02.032. Bioorg Med Chem Lett. 2004. PMID: 15080998
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