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
Docking studies
HIV-1
Noncompetitive inhibitors
Pyrimidinyl isoxazolidines
Reverse transcriptases
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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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