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Pyrrole and Fused Pyrrole Compounds with Bioactivity against Inflammatory Mediators
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Pyrrole and Fused Pyrrole Compounds with Bioactivity against Inflammatory Mediators
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Journal Article
Pyrrole and Fused Pyrrole Compounds with Bioactivity against Inflammatory Mediators
2017
Overview
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
and
, 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.
Publisher
MDPI AG,MDPI
Subject
/ Anti-Inflammatory Agents - chemical synthesis
/ Anti-Inflammatory Agents - chemistry
/ Anti-Inflammatory Agents - pharmacology
/ Anti-Inflammatory Agents, Non-Steroidal - chemical synthesis
/ Anti-Inflammatory Agents, Non-Steroidal - chemistry
/ Anti-Inflammatory Agents, Non-Steroidal - pharmacology
/ Cytokines - antagonists & inhibitors
/ Inflammation Mediators - antagonists & inhibitors
/ Inflammation Mediators - chemistry
/ Male
/ Molecular Docking Simulation
/ Molecular Dynamics Simulation
/ NMR
/ Pyrroles
/ Pyrroles - chemical synthesis
/ Rats
