Pyrrole and Fused Pyrrole Compounds with Bioactivity against Inflammatory Mediators.

Autor: Said Fatahala S; Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Helwan University, Ain-Helwan, Helwan 11795, Cairo, Egypt. samarradwan1@yahoo.com., Hasabelnaby S; Pharmaceutical Chemistry Department, Faculty of Pharmacy, Helwan University, Ain-Helwan, Helwan 11795, Cairo, Egypt. sherifajanaa@yahoo.com.; Department of Chemistry and Biochemistry, Concordia University, 7141 rue Sherbrooke O., Montréal, H4Bm1R6 QC, Canada. sherifajanaa@yahoo.com., Goudah A; Department of Pharmacology, Faculty of Veterinary Medicine, Cairo University, Giza/Egypt, Giza 12211, Egypt. aymangouda@yahoo.com., Mahmoud GI; Department of Biochemistry, Faculty of Agriculture, Cairo University, Giza/Egypt, Giza 12211, Egypt. ssfathallah@yahoo.com., Helmy Abd-El Hameed R; Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Helwan University, Ain-Helwan, Helwan 11795, Cairo, Egypt. zeiadomar@yahoo.com.
Jazyk: angličtina
Zdroj: Molecules (Basel, Switzerland) [Molecules] 2017 Mar 17; Vol. 22 (3). Date of Electronic Publication: 2017 Mar 17.
DOI: 10.3390/molecules22030461
Abstrakt: 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.
Databáze: MEDLINE
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