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ChemMedChem ; 4(2): 219-24, 2009 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-19090525

RESUMEN

A novel series of diarylpyrimidine analogues (DAPYs) featuring a naphthyl moiety at the C4 position were designed, with all compounds exhibiting strong activity against wild-type HIV-1.A novel series of diarylpyrimidine analogues (DAPYs) featuring a naphthyl moiety at the C4 position were synthesized and evaluated for their in vitro activity against HIV in MT-4 cells. All compounds exhibited strong activity against wild-type HIV-1. The most active compound showed activity against wild-type HIV-1 with an EC(50) value of 2.35 nM and against the double mutant strain (K103N+Y181C) with an EC(50) value of 6.6 microM, with a selectivity index greater than 60 000 against wild-type HIV-1. Additionally, some compounds also showed activity against HIV-2 (EC(50)=5.82 microM).


Asunto(s)
Fármacos Anti-VIH/química , Fármacos Anti-VIH/farmacología , VIH-1/efectos de los fármacos , Pirimidinas/química , Pirimidinas/farmacología , Línea Celular , Evaluación Preclínica de Medicamentos , Humanos , Espectroscopía de Resonancia Magnética , Modelos Moleculares , Estructura Molecular , Espectrometría de Masa por Ionización de Electrospray
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