Skip to main content
SpringerLink
Log in

Synthesis and pharmacological activity of the main metabolite of afobazole and its analogs

  • Published:
Pharmaceutical Chemistry Journal Aims and scope

The methods and conditions for the synthesis of the main metabolite of the selective anxiolytic afobazole, 2-[2-(3-oxomorpholin-4-yl)ethylthio]-5-ethoxybenzimidazole, and its analogs are developed. It is shown that the main metabolite demonstrates an anxiolytic effect in a dose range similar to that of afobazole. It is found that the psychopharmacological profile of the other synthesized compounds (analogs) is characterized by a less pronounced anxiolytic component.

This is a preview of subscription content, log in via an institution to check access.

Access this article

Log in via an institution

Price excludes VAT (USA)
Tax calculation will be finalised during checkout.

Instant access to the full article PDF.

Institutional subscriptions

Similar content being viewed by others

References

  1. Jpn. Pat. No. 10978; Chem. Abstr., 58, 13964f (1963).

    Google Scholar 

  2. GB Pat. No. 1,152,814; Chem. Abstr., 72, P12729u (1970).

  3. C. A. Johnson, A. Mohamond, P. Brouant, et al., Med. Chem. Res., 2(4), 247 – 255 (1992).

    CAS  Google Scholar 

  4. Jpn. Pat. No. 74 41198; Chem. Abstr., 82, P156308k (1975).

    Google Scholar 

  5. G. G. Naznamov, S. A. Syunyakov, D. V. Chumakov, et al., Psikhiatriya Psikhofarmakoter., No. 4 (8), 8 – 13 (2006).

  6. S. B. Seredenin, A. O. Viglinskaya, T. Ya. Mozhaeva, et al., Eksp. Klin. Farmakol., 71(2), 50 – 52 (2008).

    PubMed  CAS  Google Scholar 

  7. K. M. Lakin and Yu. F. Krylov, Biotransformation of Drugs [in Russian], Meditsina, Moscow (1981), pp. 23 – 24.

    Google Scholar 

  8. RF Pat. Appl. No. 2007137788; Byull. Izobret., No. 12 (2009).

  9. P. Vieles and J. Sequin, Compt. rend., 234, 1980 – 1981 (1952).

    CAS  Google Scholar 

  10. R. G. Lister, Psychopharmacol., 92, 180 – 185 (1987).

    CAS  Google Scholar 

  11. S. Pellow, P. Chopin, S. Pile, and M. Briley, J. Neurosci. Methods, 14, 149 – 167 (1985).

    Article  PubMed  CAS  Google Scholar 

  12. S. B. Seredenin, T. A. Voronina, G. G. Neznamov, et al., Vestn. Ross. Akad. Med. Nauk, 11, 3 – 9 (1998).

    PubMed  Google Scholar 

Download references

Author information

Authors and Affiliations

  1. Zakusov State Institute of Pharmacology, Russian Academy of Medical Sciences, Moscow, Russia

    T. Ya. Mozhaeva, M. A. Yarkova, V. P. Lezina & S. B. Seredenin

Authors
  1. T. Ya. Mozhaeva
    View author publications

    You can also search for this author in PubMed Google Scholar

  2. M. A. Yarkova
    View author publications

    You can also search for this author in PubMed Google Scholar

  3. V. P. Lezina
    View author publications

    You can also search for this author in PubMed Google Scholar

  4. S. B. Seredenin
    View author publications

    You can also search for this author in PubMed Google Scholar

Additional information

Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 45, No. 3, pp. 19 – 22, March, 2011.

Rights and permissions

Reprints and permissions

About this article

Cite this article

Mozhaeva, T.Y., Yarkova, M.A., Lezina, V.P. et al. Synthesis and pharmacological activity of the main metabolite of afobazole and its analogs. Pharm Chem J 45, 147–150 (2011). https://doi.org/10.1007/s11094-011-0579-x

Download citation

  • Received:

  • Published:

  • Issue Date:

  • DOI: https://doi.org/10.1007/s11094-011-0579-x

Key words

Search

Navigation