Optimization of diarylazines as anti-HIV agents with dramatically

Bollini, Mariela; Cisneros, José A.; Spasov, Krasimir A.; Anderson, Karen S.; Jorgensen, William L.

Artículos de revistas

Fecha

2013-07

Registro en:

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

0960-894X

http://hdl.handle.net/11336/24881

CONICET Digital

CONICET

http://repositorioslatinoamericanos.uchile.cl/handle/2250/1879184

Autor

Bollini, Mariela

Cisneros, José A.

Spasov, Krasimir A.

Anderson, Karen S.

Jorgensen, William L.

Institución

Consejo Nacional de Investigaciones Científicas y Tecnológicas (Argentina)

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.

Materias

Anti-HIV agent

NNRTI

Drug solubility

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