Stampidine as a novel nucleoside reverse transcriptase inhibit with potent anti-HIV activity.
Stavudine (STV, d4T, 2',3'-didehydro-3'-deoxythymidine, CAS 3056-17-5) is a standard anti-HIV drug. Stampidine (STAMP, DDE-113, HI-113, N-[p-(4-bromophenyl)-2',3'-didehydro-3'-deoxy-5'-thymidylyl]-L-alanine methyl ester, CAS 217178-62-6) is a novel aryl phosphate derivative of stavudine with more potent anti-HIV activity and more favorable pharmacodynamic features. The remarkable potency of stampidine against clinical HIV-1 isolates with NRTI- or NNRTI-resistance (NRTI, nucleoside reverse transcriptase inhibitor; NNRTI, non-nucleoside reverse transcriptase inhibitor) warrants the further development of this new anti-HIV agent.
Parker Hughes Institute, Roseville, Minnesota, USA. fatih_uckun@ih.org
Fatih M
FM
Uckun
D019380:Anti-HIV Agents / Q000009:adverse effects / Q000191:economics / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000627:therapeutic use; D002626:Chemistry, Pharmaceutical; D054306:Dideoxynucleotides; D024882:Drug Resistance, Viral; D015658:HIV Infections / Q000188:drug therapy* / Q000821:virology; D015497:HIV-1 / Q000187:drug effects; D006801:Humans; D008099:Liver / Q000187:drug effects / Q000201:enzymology*; D018894:Reverse Transcriptase Inhibitors / Q000009:adverse effects / Q000191:economics / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000627:therapeutic use; D018119:Stavudine / Q000009:adverse effects / Q000031:analogs & derivatives* / Q000191:economics / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use; D013938:Thymidine Monophosphate / Q000009:adverse effects / Q000031:analogs & derivatives* / Q000191:economics / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use
D019380:Anti-HIV Agents; D054306:Dideoxynucleotides; D018894:Reverse Transcriptase Inhibitors; C472384:stampidine; D013938:Thymidine Monophosphate; D018119:Stavudine