Novel furocoumarins as potential HIV-1 integrase inhibitors.

Olomola, Temitope O; Mosebi, Salerwe; Klein, Rosalyn; Traut-Johnstone, Telisha; Coates, Judy; Hewer, Raymond; Kaye, Perry T

Olomola, Temitope O; Mosebi, Salerwe; Klein, Rosalyn; Traut-Johnstone, Telisha; Coates, Judy; Hewer, Raymond; Kaye, Perry T.

Afiliación

Olomola TO; Department of Chemistry and Centre for Chemico- and Biomedicinal Research, Rhodes University, Grahamstown 6140, South Africa.
Mosebi S; Biomed, Advanced Materials Division, Mintek, Randburg 2125, South Africa.
Klein R; Department of Chemistry and Centre for Chemico- and Biomedicinal Research, Rhodes University, Grahamstown 6140, South Africa.
Traut-Johnstone T; Biomed, Advanced Materials Division, Mintek, Randburg 2125, South Africa.
Coates J; Biomed, Advanced Materials Division, Mintek, Randburg 2125, South Africa.
Hewer R; Biomed, Advanced Materials Division, Mintek, Randburg 2125, South Africa.
Kaye PT; Department of Chemistry and Centre for Chemico- and Biomedicinal Research, Rhodes University, Grahamstown 6140, South Africa. Electronic address: P.Kaye@ru.ac.za.

Bioorg Chem ; 57: 1-4, 2014 Dec.

Article en En | MEDLINE | ID: mdl-25159595

RESUMEN

A series of seven novel, rationally designed N-substituted 3-{3,5-dimethylfuro[3,2-g]coumarin-6-yl}propanamides have been prepared as potential HIV-1 integrase (IN) inhibitors via a five-step pathway commencing with resorcinol and diethyl 2-acetylglutarate, and the HIV-1 IN inhibition potential of these compounds has been examined relative to raltegravir, a known HIV-1 IN inhibitor.

Asunto(s)

Furocumarinas/química; Furocumarinas/farmacología; Inhibidores de Integrasa VIH/química; Inhibidores de Integrasa VIH/farmacología; VIH-1/efectos de los fármacos; Cristalografía por Rayos X; Infecciones por VIH/tratamiento farmacológico; Infecciones por VIH/enzimología; Infecciones por VIH/virología; Integrasa de VIH/química; Integrasa de VIH/metabolismo; VIH-1/enzimología; Humanos; Relación Estructura-Actividad

Palabras clave

Furocoumarins; HIV-1 integrase; Rational design; Strand-transfer inhibitors

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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Furocumarinas / VIH-1 / Inhibidores de Integrasa VIH Límite: Humans Idioma: En Revista: Bioorg Chem Año: 2014 Tipo del documento: Article País de afiliación: Sudáfrica Pais de publicación: Estados Unidos

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