000 | 03314nlm1a2200553 4500 | ||
---|---|---|---|
001 | 667752 | ||
005 | 20231030042125.0 | ||
035 | _a(RuTPU)RU\TPU\network\38963 | ||
035 | _aRU\TPU\network\38952 | ||
090 | _a667752 | ||
100 | _a20220419a2021 k y0engy50 ba | ||
101 | 0 | _aeng | |
102 | _aCH | ||
135 | _adrcn ---uucaa | ||
181 | 0 | _ai | |
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.] |
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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 |
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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 _2stltpush _3(RuTPU)RU\TPU\col\23556 |
801 | 2 |
_aRU _b63413507 _c20220419 _gRCR |
|
856 | 4 | 0 | _uhttps://doi.org/10.3390/molecules26216583 |
942 | _cCF |