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Synthesis of N-heterocyclic amides based on (+)-camphoric acid and study of their antiviral activity and pharmacokinetics

O. I. Yarovaya, D. V. Baranova,A. S. Sokolova, A. G. Nemolochnova, O. P. Sal’nikova, A. V. Fat’anova,A. D. Rogachev,A. S. Volobueva,V. V. Zarubaev,A. G. Pokrovsky,N. F. Salakhutdinov

Russian chemical bulletin = Izvestiia Akademii nauk. Seriia khimicheskaia(2023)

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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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