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182 0 _ab
200 1 _aPyridinone Derivatives as Interesting Formyl Peptide Receptor (FPR) Agonists for the Treatment of Rheumatoid Arthritis
_fL. Crocetti, C. Vergelli, G. Guerrini [et al.]
203 _aText
_celectronic
300 _aTitle screen
320 _a[References: 35 tit.]
330 _aRheumatoid 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.
461 _tMolecules
463 _tVol. 26, iss. 21
_v[6583, 22 p.]
_d2021
610 1 _aтруды учёных ТПУ
610 1 _aэлектронный ресурс
610 1 _apyridinone
610 1 _aformyl peptide receptors
610 1 _aagonists
610 1 _arheumatoid arthritis
610 1 _amolecular docking
610 1 _aагонисты
610 1 _aревматоидный артрит
610 1 _aлечение
610 1 _aхронические заболевания
701 1 _aCrocetti
_bL.
_gLetizia
701 1 _aVergelli
_bC.
_gClaudia
701 1 _aGuerrini
_bG.
_gGabriella
701 1 _aGiovannoni
_bM. P.
_gMaria Paola
701 1 _aKirpotina
_bL. N.
_gLiliya Nikolaevna
701 1 _aKhlebnikov
_bA. I.
_cChemist
_cProfessor of Tomsk Polytechnic University
_f1963-
_gAndrey Ivanovich
_2stltpush
_3(RuTPU)RU\TPU\pers\33927
701 1 _aGhelardini
_bC.
_gCarla
701 0 _aMannelli Lorenzo Di Cesare
701 1 _aLucarini
_bE.
_gElena
701 1 _aShchepyotkin
_bI. A.
_gIgor Aleksandrovich
701 1 _aQuinn
_bM. T.
_gMark
712 0 2 _aНациональный исследовательский Томский политехнический университет
_bИнженерная школа новых производственных технологий
_bНаучно-образовательный центр Н. М. Кижнера
_h7872
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856 4 0 _uhttps://doi.org/10.3390/molecules26216583
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