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

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 t...

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Veröffentlicht in:Russian chemical bulletin 2023, Vol.72 (3), p.807-818
Hauptverfasser: Yarovaya, O. I., Baranova, D. V., Sokolova, A. S., Nemolochnova, A. G., Sal’nikova, O. P., Fat’anova, A. V., Rogachev, A. D., Volobueva, A. S., Zarubaev, V. V., Pokrovsky, A. G., Salakhutdinov, N. F.
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Sprache:eng
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Zusammenfassung: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.
ISSN:1066-5285
1573-9171
DOI:10.1007/s11172-023-3845-9