Skip to main content
SpringerLink
Log in

Influence of urea-equivalent groups in position 5 of 2-amino, 2-(1-aminoethylidenamino) and 2-guanidino thiazole derivatives on H2-receptor antagonist activity in gastric fistula cat

  • Histamine and the Gastrointestinal Tract
  • Published:
Agents and Actions Aims and scope Submit manuscript

Abstract

A series of thiazole derivatives, in which a side-chain with different urea-equivalent groups was introduced in position 5 of the heterocycle, have been tested as inhibitors of dimaprit-induced gastric acid and pepsin secretion in the gastric fistula cat. By comparing thein vivo and the previously reportedin vitro activity of these compounds, we can note a very close parallelism not only in the quality of their action but also in the estimates of pA2 values. These data support an interdependence between the molecular substructures and the affinity for the H2-receptor.

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. E. Barocelli, M. Chiavarini, G. Morini, P. V. Plazzi, T. Vitali and M. Impicciatore,H 2-receptor antagonist activity of N-methylthiourea, N-cyano-N′-methylguanidine, N-cyanoamidine, N-carbamoylamidine and N-sulfamoylamidine 5-substituted thiazole derivatives on guinea pig atria. Agents and Actions27, 195–197 (1989).

    PubMed  Google Scholar 

  2. I. Yanagisawa, Y. Hirata and Y. Ishii,Histamine H 2-receptor antagonists. 1. Synthesis of N-cyano and N-carbamoyl amidine derivatives and their biological activities. J. med. Chem.27, 849–857 (1984).

    PubMed  Google Scholar 

  3. I. Yanagisawa, Y. Hirata and Y. Ishii,Studies on histamine H 2-receptor antagonists. 2. Synthesis and pharmacological activities of N-sulfamoyl and N-sulfonyl amidine derivatives. J. med. Chem.30, 1787–1793 (1987).

    PubMed  Google Scholar 

  4. C. R. Ganellin,Chemistry and structure-activity relationships of drugs acting at histamine receptors. InPharmacology of histamine receptors. (Eds. C. R. Ganellin and M. E. Parsons) pp. 10–102, Wright PSG, Bristol 1982.

    Google Scholar 

Download references

Author information

Authors and Affiliations

  1. Institute of Pharmacology and Pharmacognosy, University of Parma, Parma, Italy

    M. Chiavarini, G. Morini, E. Barocelli &  M. Impicciatore

  2. Institute of Pharmaceutical Chemistry, Department of Pharmacy, University of Parma, Via Massimo D'Azeglio 85, 43100, Parma, Italy

    F. Bordi, P. V. Plazzi & T. Vitali

Authors
  1. M. Chiavarini
    View author publications

    You can also search for this author in PubMed Google Scholar

  2. G. Morini
    View author publications

    You can also search for this author in PubMed Google Scholar

  3. E. Barocelli
    View author publications

    You can also search for this author in PubMed Google Scholar

  4. F. Bordi
    View author publications

    You can also search for this author in PubMed Google Scholar

  5. P. V. Plazzi
    View author publications

    You can also search for this author in PubMed Google Scholar

  6. T. Vitali
    View author publications

    You can also search for this author in PubMed Google Scholar

  7. M. Impicciatore
    View author publications

    You can also search for this author in PubMed Google Scholar

Rights and permissions

Reprints and permissions

About this article

Cite this article

Chiavarini, M., Morini, G., Barocelli, E. et al. Influence of urea-equivalent groups in position 5 of 2-amino, 2-(1-aminoethylidenamino) and 2-guanidino thiazole derivatives on H2-receptor antagonist activity in gastric fistula cat. Agents and Actions 27, 192–194 (1989). https://doi.org/10.1007/BF02222236

Download citation

  • Issue Date:

  • DOI: https://doi.org/10.1007/BF02222236

Keywords

Search

Navigation