Modified 2,3-dideoxynucleosides for treatment infections caused by human immunodeficiency virus (HIV) multidrug resistant strains, method of their synthesis and the pharmaceutical agent containing these nucleosides
2,3-Dideoxy-3-fluoro-4-thiothymidine (4-SFLT) derivatives according to the invention substituted at 5-O position of 4-SFLT with 12-tetradodecanoyl, 12-bromododecanoyl, 12-metoxydodecanoyl, 12-ethylothiododecanoyl, 11-ethylothioundecanoyl or 12-azidodocanoyl group (represented by the symbols WA18, WA19, WA21,WA22,WA23 and WA20 in the deCIPhR™ cell system exert high antiviral activity against wild type HIV-1 strain, as well as against its drug and multidrug resistant strains, and moreover very low citotoxicity (CC50 > 200 µM) and very high selectivity.The compounds, because of lack of toxicity may be applied at all AIDS phases i.e. also them the T4 lymphocytes level in patients drops down below 200/ µL of peripheral blood.2,3-Dideoxy-3-fluoro-4-thiothymidine derivatives according to the invention are synthesized by the transformation of the known compound 2,3-dideoxy-3-fluoro-4-thiothymidine (4-SFLT).
