4,5-Dihydroxypyrimidine carboxamides and N-alkyl-5-hydroxypyrimidinone carboxamides are potent, selective HIV integrase inhibitors with good pharmacokinetic profiles in preclinical species

Journal of Medicinal Chemistry

Volumn 49, Issue 23, 2006, Pages 6646-6649

  Summa, Vincenzo ^a   Petrocchi, Alessia ^a   Matassa, Victor G ^a,b   Gardelli, Cristina ^a   Muraglia, Ester ^a   Rowley, Michael ^a   Paz, Odalys Gonzalez ^a   Laufer, Ralph ^a   Monteagudo, Edith ^a   Pace, Paola ^a  

^a IRBM   (Italy)

^b Almirall Prodesfarma S A   (Spain)

Author keywords

[No Author keywords available]

Indexed keywords

ALKYL GROUP; AMIDE; INTEGRASE; INTEGRASE INHIBITOR; PYRIMIDINE DERIVATIVE; PYRIMIDINONE DERIVATIVE;

ANTIVIRAL ACTIVITY; AREA UNDER THE CURVE; ARTICLE; DOG; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG HALF LIFE; DRUG POTENCY; DRUG PROTEIN BINDING; DRUG SELECTIVITY; HUMAN; IC 50; LIPOPHILICITY; NONHUMAN; NORMAL HUMAN; PHYSICAL CHEMISTRY; PLASMA CLEARANCE; RAT; RHESUS MONKEY; STRUCTURE ACTIVITY RELATION;

ADMINISTRATION, ORAL; AMIDES; ANIMALS; BIOLOGICAL AVAILABILITY; DOGS; HIV INTEGRASE INHIBITORS; HIV-1; HUMANS; MACACA MULATTA; PYRIMIDINES; PYRIMIDINONES; RATS; SERUM; STRUCTURE-ACTIVITY RELATIONSHIP; VIRUS REPLICATION;

EID: 33751014050     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm060854f     Document Type: Article

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