The potential of aspirin in prodrug synthesis A new potential delivery system of AZT and FLT /
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 nucleosid...
Elmentve itt :
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| Dokumentumtípus: | Cikk |
| Megjelent: |
1996
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| Sorozat: | ARCHIV DER PHARMAZIE
329 No. 8-9 |
| Tárgyszavak: | |
| doi: | 10.1002/ardp.19963290809 |
| mtmt: | 1505911 |
| Online Access: | http://publicatio.bibl.u-szeged.hu/31831 |
| Tartalmi kivonat: | 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. |
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| Terjedelem/Fizikai jellemzők: | 417-420 |
| ISSN: | 0365-6233; 1521-4148 |