Affairs of the HAART! The synthesis of HEPT-derived, truncated reverse isoxazolidinyl nucleosides ( shown) is reported. These compounds represent the first examples of isoxazolidines bearing a pyrimidine scaffold at the C-3 position using a glycoside-type linkage. Biological evaluation showed that some of the derivatives act as non-nucleoside inhibitors of HIV-1 reverse transcriptase, with an efficacy comparable to that of Nevirapine but with reduced toxicity.

Truncated Reverse Isoxazolidinyl Nucleosides: A New Class of Allosteric HIV-1 Reverse Transcriptase Inhibitors

Mastino A;
2012

Abstract

Affairs of the HAART! The synthesis of HEPT-derived, truncated reverse isoxazolidinyl nucleosides ( shown) is reported. These compounds represent the first examples of isoxazolidines bearing a pyrimidine scaffold at the C-3 position using a glycoside-type linkage. Biological evaluation showed that some of the derivatives act as non-nucleoside inhibitors of HIV-1 reverse transcriptase, with an efficacy comparable to that of Nevirapine but with reduced toxicity.
2012
FARMACOLOGIA TRASLAZIONALE - IFT
Inglese
7
4
565
569
5
http://www.scopus.com/inward/record.url?eid=2-s2.0-84859183544&partnerID=q2rCbXpz
Sì, ma tipo non specificato
Docking studies
HIV-1
Noncompetitive inhibitors
Pyrimidinyl isoxazolidines
Reverse transcriptases
9
info:eu-repo/semantics/article
262
Romeo, R; Giofre, Sv; Macchi, B; Balestrieri, E; Mastino, A; Merino, P; Carnovale, C; Romeo, G; Chiacchio, U
01 Contributo su Rivista::01.01 Articolo in rivista
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/20.500.14243/310808
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