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 |
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Hauptverfasser: | , , , , , , , , , , |
Format: | Artikel |
Sprache: | eng |
Schlagworte: | |
Online-Zugang: | Volltext |
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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. |
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ISSN: | 1066-5285 1573-9171 |
DOI: | 10.1007/s11172-023-3845-9 |