SYNTHESIS AND ANTI-HIV ACTIVITY OF NEW HOMO ACYCLIC NUCLEOSIDES, 1-(PENT-4-ENYL)QUINOXALIN-2-ONES AND 2-(PENT-4-ENYLOXY)QUINOXALINES
DOI:
https://doi.org/10.1007/7426Keywords:
acyclonucleosides, glycosides, quinoxalines, alkylation, antiviral activityAbstract
A series of acyclonucleosides 6,7-disubstituted 1-(pent-4-enyl)quinoxalin-2-one derivatives and the O-analogs were synthesized by a one-step condensation of the corresponding quinoxaline bases with 5-bromo-1-pentene. Acyclonucleosides prepared were assayed against HIV-1 and HIV-2 in MT-4 cells. 6,7-Dimethyl-2-(pent-4-enyloxy)quinoxaline showed inhibition of HIV-1
with EC50 value of 0.22 ± 0.08 µg/ml and a therapeutic index of 13. This means that it was cytotoxic to MT-4 cells at CC50 of 2.6 ± 0.1 µg/ml.
How to Cite
Ali, I. A. I.; Al-Masoudi, I. A.; Hassan, H. Gh.; Al-Masoudi, N. A. Chem. Heterocycl. Compd. 2007, 43, 1052. [Khim. Geterotsikl. Soedin. 2007, 1243.]
For this article in the English edition see DOI 10.1007/s10593-007-0164-0