Pyridinone Derivatives as Interesting Formyl Peptide Receptor (FPR) Agonists for the Treatment of Rheumatoid Arthritis

Pyridinone Derivatives as Interesting Formyl Peptide Receptor (FPR) Agonists for the Treatment of Rheumatoid Arthritis

Bibliographic Details
Parent link:Molecules
Vol. 26, iss. 21.— 2021.— [6583, 22 p.]
Corporate Author: Национальный исследовательский Томский политехнический университет Инженерная школа новых производственных технологий Научно-образовательный центр Н. М. Кижнера
Other Authors: Crocetti L. Letizia, Vergelli C. Claudia, Guerrini G. Gabriella, Giovannoni M. P. Maria Paola, Kirpotina L. N. Liliya Nikolaevna, Khlebnikov A. I. Andrey Ivanovich, Ghelardini C. Carla, Mannelli Lorenzo Di Cesare, Lucarini E. Elena, Shchepyotkin I. A. Igor Aleksandrovich, Quinn M. T. Mark
Summary:Title screen
Rheumatoid arthritis (RA) is a chronic inflammatory disease characterized by joint inflammation, cartilage damage and bone destruction. Although the pharmacological treatment of RA has evolved over the last few years, the new drugs have serious side effects and are very expensive. Thus, the research has been directed in recent years towards new possible targets. Among these targets, N-formyl peptide receptors (FPRs) are of particular interest. Recently, the mixed FPR1/FPR2 agonist Cpd43, the FPR2 agonist AT-01-KG, and the pyridine derivative AMC3 have been shown to be effective in RA animal models. As an extension of this research, we report here a new series of pyridinone derivatives containing the (substituted)phenyl acetamide chain, which was found to be essential for activity, but with different substitutions at position 5 of the scaffold. The biological results were also supported by molecular modeling studies and additional pharmacological tests on AMC3 have been performed in a rat model of RA, by repeating the treatments of the animals with 10 mg/kg/day of compound by 1 week.
Language:English
Published: 2021
Subjects:
труды учёных ТПУ
электронный ресурс
pyridinone
formyl peptide receptors
agonists
rheumatoid arthritis
molecular docking
агонисты
ревматоидный артрит
лечение
хронические заболевания
Online Access:https://doi.org/10.3390/molecules26216583
Format: Electronic Book Chapter
KOHA link:https://koha.lib.tpu.ru/cgi-bin/koha/opac-detail.pl?biblionumber=667752

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