Design and synthesis of bicyclic pyrimidinones as potent and orally bioavailable HIV-1 integrase inhibitors

Journal of Medicinal Chemistry

Volumn 51, Issue 4, 2008, Pages 861-874

  Muraglia, Ester ^a   Kinzel, Olaf ^a   Gardelli, Cristina ^a   Crescenzi, Benedetta ^a   Donghi, Monica ^a   Ferrara, Marco ^a   Nizi, Emanuela ^a   Orvieto, Federica ^a   Pescatore, Giovanna ^a   Laufer, Ralph ^a   Gonzalez Paz, Odalys ^a   Di Marco, Annalise ^a   Fiore, Fabrizio ^a   Monteagudo, Edith ^a   Fonsi, Massimiliano ^a   Felock, Peter J ^b   Rowley, Michael ^a   Summa, Vincenzo ^a  

^a Merck Research Laboratories   (Italy)

^b MERCK RESEARCH LABORATORIES   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

INTEGRASE INHIBITOR; PYRIMIDINONE DERIVATIVE; SULFONAMIDE;

ARTICLE; CELL CULTURE; CONTROLLED STUDY; DRUG ACTIVITY; DRUG BIOAVAILABILITY; DRUG DESIGN; DRUG MARKETING; DRUG STRUCTURE; DRUG SUBSTITUTION; DRUG SYNTHESIS; GENOME; HUMAN; HUMAN CELL; HUMAN IMMUNODEFICIENCY VIRUS INFECTION; IC 50; PHYSICAL CHEMISTRY; STRUCTURE ACTIVITY RELATION; VIRUS INHIBITION; VIRUS REPLICATION;

ADMINISTRATION, ORAL; AMINOPYRIDINES; ANIMALS; AZEPINES; BICYCLO COMPOUNDS, HETEROCYCLIC; BIOLOGICAL AVAILABILITY; CELL LINE; DOGS; HIV INTEGRASE; HIV INTEGRASE INHIBITORS; HIV-1; HUMANS; MACACA MULATTA; MICROSOMES, LIVER; PYRIMIDINONES; RATS; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 39749089270     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm701164t     Document Type: Article

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35. Synthesis described in the Supporting Information.
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