4.6 Article

Pyrrole and Fused Pyrrole Compounds with Bioactivity against Inflammatory Mediators

Journal

MOLECULES
Volume 22, Issue 3, Pages -

Publisher

MDPI
DOI: 10.3390/molecules22030461

Keywords

pyrroles; pyrrolopyridines; synthesis; anti-inflammatory assay; cytokine inhibitors; docking study

Funding

  1. Pharmaceutical Organic Chemistry
  2. Faculty of Pharmacy, Helwan University

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A new series of pyrrolopyridines and pyrrolopyridopyrimidines have been synthesized from aminocyanopyrroles. The synthesized compounds have been characterized by FTIR, H-1-NMR and mass spectroscopy. The final compounds have been screened for in vitro pro-inflammatory cytokine inhibitory and in vivo anti-inflammatory activity. The biological results revealed that among all tested compounds some fused pyrroles, namely the pyrrolopyridines 3i and 3l, show promising activity. A docking study of the active synthesized molecules confirmed the biological results and revealed a new binding pose in the COX-2 binding site.

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