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Truncated Reverse Isoxazolidinyl Nucleosides: A New Class of Allosteric HIV‐1 Reverse Transcriptase Inhibitors
Author(s) -
Romeo Roberto,
Giofrè Salvatore V.,
Macchi Beatrice,
Balestrieri Emanuela,
Mastino Antonio,
Merino Pedro,
Carnovale Caterina,
Romeo Giovanni,
Chiacchio Ugo
Publication year - 2012
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201200022
Subject(s) - reverse transcriptase , nevirapine , human immunodeficiency virus (hiv) , nucleoside reverse transcriptase inhibitor , stereochemistry , nucleoside , chemistry , nucleoside analogue , pyrimidine , computational biology , combinatorial chemistry , virology , computer science , biology , biochemistry , rna , antiretroviral therapy , gene , viral load
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.