Aza TSAO-T derivatives bearing a dihydroisothiazole dioxide ring instead of an oxathiole dioxidering at the C-3‘ position on the sugar moiety were prepared. We have synthesized four familiesof compounds depending on substitution at both N-3 and N-2‘ ‘. Biological evaluation showedthat these compounds are HIV-1(IIIB)-specific and potent reverse transcriptase inhibitors withEC50 values between 0.13 and 3.5 μM in cell culture.
