New condensed pyrroles of potential biological interest syntheses and structure-activity relationship studies

Eur J Med Chem. 2011 Jul;46(7):3022-9. doi: 10.1016/j.ejmech.2011.04.034. Epub 2011 Apr 16.

Abstract

The Pyrrole derivatives Ia-d were prepared and utilized for the preparation of pyrrolo[2,3-d]pyrimidine derivatives IIa-c, III, IVa-e, V and VIIIa-c; pyrrolo[3,2-e]tetrazolo[1,5-c]pyrimidine VI and pyrrolo[4,3e][1,2,4]triazolo[1,5-c]pyrimidine derivative derivatives VIIa-c. These some newly synthesized compounds were examined for their in vitro antimicrobial activity and in vivo anti-inflammatory. Result indicated that these compounds showed promising anti-inflammatory activity in comparison to ibuprofen (the standard anti-inflammatory drug). The structure-activity relationships (SAR) and anti-inflammatory activities of these compounds are also discussed in this paper.

MeSH terms

  • Animals
  • Anti-Bacterial Agents / chemical synthesis*
  • Anti-Bacterial Agents / pharmacology
  • Anti-Inflammatory Agents, Non-Steroidal / chemical synthesis*
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacology
  • Bacillus subtilis / drug effects
  • Bacillus subtilis / growth & development
  • Carrageenan
  • Edema / chemically induced
  • Edema / drug therapy*
  • Edema / pathology
  • Hindlimb
  • Ibuprofen / pharmacology
  • Male
  • Microbial Sensitivity Tests
  • Pyrimidines / chemical synthesis*
  • Pyrimidines / pharmacology
  • Pyrroles / chemical synthesis*
  • Pyrroles / pharmacology
  • Rats
  • Rats, Sprague-Dawley
  • Staphylococcus aureus / drug effects
  • Staphylococcus aureus / growth & development
  • Structure-Activity Relationship

Substances

  • Anti-Bacterial Agents
  • Anti-Inflammatory Agents, Non-Steroidal
  • Pyrimidines
  • Pyrroles
  • Carrageenan
  • Ibuprofen