Synthesis of N-heterocyclic amides based on (+)-camphoric acid and study of their antiviral activity and pharmacokinetics
Russian chemical bulletin = Izvestiia Akademii nauk. Seriia khimicheskaia(2023)
摘要
Efficient conditions for the synthesis of nitrogen-containing heterocyclic derivatives of (1 R ,3 S )(+)-camphoric acid were selected. A series of heterocyclic compounds based on (+)-camphoric acid bearing pharmacophoric fragments was synthesized using the developed methodology. The compounds were tested for their antiviral activity against SARS-CoV-2 and H1N1 influenza viruses, and efficient inhibitors were identified that are of significant interest for further studies. The stability of the compounds and pharmaco-kinetics of the leader compound were studied when administered intragastrically and intramuscularly to mice at a dose of 200 mg kg −1 using the HPLC-MS/MS method.
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关键词
(+)-camphoric acid,N-heterocycles,A H1N1 influenza virus,SARS-CoV-2 virus,pharmacokinetics
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