Conclusions
The new anti-AIDS agents, polyrotaxane-AZT conjugates, were synthesized from 3′-azido-3′-deoxythymidine (AZT) and succinic anhydride, followed by condensation reactions to be conjugated with polyrotaxane, which was prepared from PEG and α-CD. The number of α-CDs in polyrotaxane was determined to be ca. 15 from1H NMR and UV spectra. The degree of AZT substitution per one conjugate molecule ranged from 1.4 to 3.2 based on elemental analysis.In vitro anti-AIDS activities, the CC50 values of the synthesized conjugates were much greater than that of AZT, and their SI values were as effective as that of AZT. This research describes novel structures that may have potential applications in drug delivery system for anti-AIDS drugs.