Related Experiment Video
Updated: Jul 8, 2026

Quantitative Structure-Activity Relationship, Activity Prediction, and Molecular Dynamics of Non-nucleotide Reverse Transcriptase Inhibitors
Published on: May 9, 2025
New acyclic quinoxaline nucleosides. Synthesis and anti-hiv activity
Ibrahim A I Ali1, Iman A Al-Masoudi, Nazik M Aziz
1Department of Chemistry, Faculty of Science, Suez Canal University, Ismailia, Egypt.
Abstract:
A series of acyclonucleosides substituted 1-(4,5-dihydroxypentyl) (13-8) and 2-(4,5-dihydroxypentyloxy)quinoxalines (19-24) were synthesized by the sharpless asymmetric dihydroxylation of the derivatives 1-6 and 7-12, respectively. Treatment of the quinoxaline base 26 with (R)-2,2-dimethyl-1,3-dioxolan-4-ylmethyl-p-toluenesulfonate (27) in the presence of NaH/DMF furnished 28. Acid hydrolysis of 28 gave 1-(2,3-dihydroxypropyl)-6,7-dimethyl-quinoxaline-2-one (29). Alternatively, 29 was prepared by sharpless dihydroxylation of 30. All the compounds were evaluated for their in vitro anti-HIV-1 and HIV-2 in MT-4 cell and found inactive, except 29, which showed inhibition of HIV-1 with EC50 value of 0.15 +/- 0.1 microg/ml and a therapeutic index (SI) of 73.
Related Concept Videos
Antiviral Nucleoside Inhibitors
Inhibitors of Viral Protein Synthesis
Inhibitors of Virion Maturation and Assembly
Retrovirus Life Cycles
Inhibitors of Bacterial DNA Synthesis
Inhibitors Of Virion Release

