info:eu-repo/semantics/article
Picomolar inhibitors of HIV-1 reverse transcriptase: Design and crystallography of naphthyl phenyl ethers
Fecha
2014-11Registro en:
Won-Gil Lee; Frey, Kathleen M.; Ricardo Gallardo-Macias; Spasov, Krasimir A.; Bollini, Mariela; et al.; Picomolar inhibitors of HIV-1 reverse transcriptase: Design and crystallography of naphthyl phenyl ethers; American Chemical Society; ACS Medicinal Chemistry Letters; 5; 11; 11-2014; 1259-1262
1948-5875
CONICET Digital
CONICET
Autor
Won-Gil Lee
Frey, Kathleen M.
Ricardo Gallardo-Macias
Spasov, Krasimir A.
Bollini, Mariela
Anderson, Karen S.
Jorgensen, William L.
Resumen
Catechol diethers that incorporate a 6-cyano-1-naphthyl substituent have been explored as non-nucleoside inhibitors of HIV-1 reverse transcriptase (NNRTIs). Promising compounds are reported that show midpicomolar activity against the wild-type virus and sub-20 nM activity against viral variants bearing Tyr181Cys and Lys103Asn mutations in HIV-RT. An X-ray crystal structure at 2.49 Å resolution is also reported for the key compound 6e with HIV-RT.