%X Aspirin (O-acetylsalicylic acid) has been used to synthesize prodrugs of 3'-azido-3'-deoxythymidine (AZT) and 3'-deoxy-3'-fluorothymidine (FLT). The mixed anhydride between aspirin and trifluoroacetic acid was synthesized and reacted with AZT and FLT to give the blocked nucleosides attached through the 5'-O position to the 2-position of 2-methyl-4H-1,3-benzodioxin-4-one. The prodrugs showed the same activities against HIV-1 in MT-4 cells as the original drugs. Hydrolysis of the synthesized prodrugs in the growth medium, used for anti-HIV investigations, resulted in formation of 5-O acetylated drugs which were subsequently hydrolyzed into the original drugs.
%I mi
%O Nincs jelölve levelező szerzőség a közleményen. (TP, SZTE admin5)
%R MTMT:1505911 10.1002/ardp.19963290809
%J ARCHIV DER PHARMAZIE
%N 8-9
%D 1996
%P 417-420
%V 329
%A  Zahran Magdy A.
%A  KovĂĄcs Lajos
%A  ElSakka Ibrahim
%A  Pedersen Erik B.
%A  Nielsen Claus
%T The potential of aspirin in prodrug synthesis: A new potential delivery system of AZT and FLT
%L publicatio31831