Artículo
Optimization of diarylazines as anti-HIV agents with dramatically
Bollini, Mariela
; Cisneros, José A.; Spasov, Krasimir A.; Anderson, Karen S.; Jorgensen, William L.
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Fecha de publicación:
07/2013
Editorial:
Elsevier
Revista:
Bioorganic & Medicinal Chemistry Letters
ISSN:
0960-894X
Idioma:
Inglés
Tipo de recurso:
Artículo publicado
Clasificación temática:
Resumen
Non-nucleoside inhibitors of HIV-1 reverse transcriptase are reported that have ca. 100-fold greater solubility than the structurally related drugs etravirine and rilpivirine, while retaining high anti-viral activity. The solubility enhancements come from strategic placement of a morpholinylalkoxy substituent in the entrance channel of the NNRTI binding site. Compound 4d shows low-nanomolar activity similar to etravirine towards wild-type HIV-1 and key viral variants.
Palabras clave:
Anti-Hiv Agent
,
Nnrti
,
Drug Solubility
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Articulos(SEDE CENTRAL)
Articulos de SEDE CENTRAL
Articulos de SEDE CENTRAL
Citación
Bollini, Mariela; Cisneros, José A.; Spasov, Krasimir A.; Anderson, Karen S.; Jorgensen, William L.; Optimization of diarylazines as anti-HIV agents with dramatically; Elsevier; Bioorganic & Medicinal Chemistry Letters; 23; 18; 7-2013; 5213-5216
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