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Synthesis and Antimicrobial Activity of Novel Heterocyclic Sulfamoyl-phenyl-carboximidamides Derived from Clinically Applied Sulfonamides

  1. Katarzyna Gobis1,*,
  2. Henryk Foks1,
  3. Katarzyna Wiśniewska2,
  4. Maria Dąbrowska-Szponar2,
  5. Ewa Augustynowicz-Kopeć3,
  6. Agnieszka Napiórkowska3

Article first published online: 7 AUG 2012

DOI: 10.1002/ardp.201200160

Issue

Archiv der Pharmazie

Archiv der Pharmazie

Volume 345, Issue 11, pages 911–917, November 2012

Additional Information

How to Cite

Gobis, K., Foks, H., Wiśniewska, K., Dąbrowska-Szponar, M., Augustynowicz-Kopeć, E. and Napiórkowska, A. (2012), Synthesis and Antimicrobial Activity of Novel Heterocyclic Sulfamoyl-phenyl-carboximidamides Derived from Clinically Applied Sulfonamides. Arch. Pharm. Pharm. Med. Chem., 345: 911–917. doi: 10.1002/ardp.201200160

Author Information

  1. 1

    Department of Organic Chemistry, Medical University of Gdańsk, Poland

  2. 2

    Department of Medicinal Microbiology, Chair of Microbiology, Medical University of Gdańsk, Poland

  3. 3

    Department of Microbiology, Institute of Tuberculosis and Pulmonary Diseases, Warsaw, Poland

*Department of Organic Chemistry, Medical University of Gdańsk, 107 Gen. Hallera Ave., 80-416 Gdansk, Poland. Fax: +48 58 349 31 45.

Publication History

  1. Issue published online: 2 NOV 2012
  2. Article first published online: 7 AUG 2012
  3. Manuscript Accepted: 29 JUN 2012
  4. Manuscript Revised: 21 JUN 2012
  5. Manuscript Received: 17 APR 2012

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Keywords:

  • Antimicrobial activity;
  • Methyl cabimidates;
  • SAR analysis;
  • Sulfonamides;
  • Synthesis

Abstract

A series of novel heterocyclic sulfamoyl-phenyl-carboximidamides were synthesized in satisfactory yields via condensation of clinically applied sulfonamides with heterocyclic methyl carbimidates. New structures were confirmed by IR and NMR spectra as well as elemental analyses. All the compounds were screened for their antibacterial, antifungal, and tuberculostatic activities. Preliminary results indicated that some target compounds exhibited promising antibacterial potency. Especially, N-[4-(thiazol-2-sulfamoyl)phenyl]pyrazine-2-carboximidamide (16) was found to be as potent as clinically applied sulfamethoxypyridazine.

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