Pyrrole and fused pyrrole compounds with bioactivity against inflammatory mediators

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Abstract

A new series of pyrrolopyridines and pyrrolopyridopyrimidines have been synthesized from aminocyanopyrroles. The synthesized compounds have been characterized by FTIR, 1H-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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Fatahala, S. S., Hasabelnaby, S., Goudah, A., Mahmoud, G. I., Abd-El Hameed, R. H., & Muñoz-Torrero, D. (2017). Pyrrole and fused pyrrole compounds with bioactivity against inflammatory mediators. Molecules, 22(3). https://doi.org/10.3390/molecules22030461

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