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Synthesis of N-heterocyclic amides based on (+)-camphoric acid and study of their antiviral activity and pharmacokinetics.
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.
  • Yarovaya OI; N. N. Vorozhtsov Novosibirsk Institute of Organic Chemistry, Siberian Branch of the Russian Academy of Sciences, 9 prosp. Akademika Lavrent'eva, 630090 Novosibirsk, Russian Federation.
  • Baranova DV; Novosibirsk State University, 2 ul. Pirogova, 630090 Novosibirsk, Russian Federation.
  • Sokolova AS; N. N. Vorozhtsov Novosibirsk Institute of Organic Chemistry, Siberian Branch of the Russian Academy of Sciences, 9 prosp. Akademika Lavrent'eva, 630090 Novosibirsk, Russian Federation.
  • Nemolochnova AG; N. N. Vorozhtsov Novosibirsk Institute of Organic Chemistry, Siberian Branch of the Russian Academy of Sciences, 9 prosp. Akademika Lavrent'eva, 630090 Novosibirsk, Russian Federation.
  • Sal'nikova OP; N. N. Vorozhtsov Novosibirsk Institute of Organic Chemistry, Siberian Branch of the Russian Academy of Sciences, 9 prosp. Akademika Lavrent'eva, 630090 Novosibirsk, Russian Federation.
  • Fat'anova AV; Novosibirsk State University, 2 ul. Pirogova, 630090 Novosibirsk, Russian Federation.
  • Rogachev AD; Novosibirsk State University, 2 ul. Pirogova, 630090 Novosibirsk, Russian Federation.
  • Volobueva AS; Novosibirsk State University, 2 ul. Pirogova, 630090 Novosibirsk, Russian Federation.
  • Zarubaev VV; N. N. Vorozhtsov Novosibirsk Institute of Organic Chemistry, Siberian Branch of the Russian Academy of Sciences, 9 prosp. Akademika Lavrent'eva, 630090 Novosibirsk, Russian Federation.
  • Pokrovsky AG; Novosibirsk State University, 2 ul. Pirogova, 630090 Novosibirsk, Russian Federation.
  • Salakhutdinov NF; Pasteur Institute of Epidemiology and Microbiology, 14 ul. Mira, 197101 St. Petersburg, Russian Federation.
Russ Chem Bull ; 72(3): 807-818, 2023.
Article in English | MEDLINE | ID: covidwho-2306106
ABSTRACT
Efficient conditions for the synthesis of nitrogen-containing heterocyclic derivatives of (1R,3S)(+)-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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Full text: Available Collection: International databases Database: MEDLINE Language: English Journal: Russ Chem Bull Year: 2023 Document Type: Article

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Full text: Available Collection: International databases Database: MEDLINE Language: English Journal: Russ Chem Bull Year: 2023 Document Type: Article