Discovery of Raltegravir, a potent, selective orally bioavailable HIV-integrase inhibitor for the treatment of HIV-AIDS infection

Human immunodeficiency virus type-1 (HIV-1) integrase is one of the three virally encoded enzymes required for replication and therefore a rational target for chemotherapeutic intervention in the treatment of HIV-1 infection. We report here the discovery of Raltegravir, the first HIV-integrase inhib...

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Veröffentlicht in:	Journal of medicinal chemistry Jg. 51; H. 18; S. 5843 - 5855
Hauptverfasser:	Summa, Vincenzo, Petrocchi, Alessia, Bonelli, Fabio, Crescenzi, Benedetta, Donghi, Monica, Ferrara, Marco, Fiore, Fabrizio, Gardelli, Cristina, Paz, Odalys Gonzalez, Hazuda, Daria J., Jones, Philip, Kinzel, Olaf, Laufer, Ralph, Monteagudo, Edith, Muraglia, Ester, Nizi, Emanuela, Orvieto, Federica, Pace, Paola, Pescatore, Giovanna, Scarpelli, Rita, Stillmock, Kara, Witmer, Marc V., Rowley, Michael
Format:	Journal Article
Sprache:	Englisch
Veröffentlicht:	WASHINGTON Amer Chemical Soc 25.09.2008
Schlagworte:	Administration, Oral Area Under Curve Biological Availability Chemistry, Medicinal Half-Life HIV Infections - drug therapy HIV Integrase Inhibitors - administration & dosage HIV Integrase Inhibitors - pharmacokinetics HIV Integrase Inhibitors - pharmacology HIV Integrase Inhibitors - therapeutic use Humans Life Sciences & Biomedicine Magnetic Resonance Spectroscopy Mass Spectrometry Pharmacology & Pharmacy Pyrrolidinones - administration & dosage Pyrrolidinones - pharmacokinetics Pyrrolidinones - pharmacology Pyrrolidinones - therapeutic use Raltegravir Potassium Science & Technology CELLS DESIGN DEPENDENT RNA-POLYMERASE REPLICATION 4,5-DIHYDROXYPYRIMIDINE ACIDS
ISSN:	0022-2623, 1520-4804, 1520-4804
Online-Zugang:	Weitere Angaben
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