Pyridinone Derivatives as Interesting Formyl Peptide Receptor (FPR) Agonists for the Treatment of Rheumatoid Arthritis
| Parent link: | Molecules Vol. 26, iss. 21.— 2021.— [6583, 22 p.] |
|---|---|
| সংস্থা লেখক: | |
| অন্যান্য লেখক: | , , , , , , , , , , |
| সংক্ষিপ্ত: | 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. |
| প্রকাশিত: |
2021
|
| বিষয়গুলি: | |
| অনলাইন ব্যবহার করুন: | https://doi.org/10.3390/molecules26216583 |
| বিন্যাস: | বৈদ্যুতিক গ্রন্থের অধ্যায় |
| KOHA link: | https://koha.lib.tpu.ru/cgi-bin/koha/opac-detail.pl?biblionumber=667752 |
MARC
| LEADER | 00000naa0a2200000 4500 | ||
|---|---|---|---|
| 001 | 667752 | ||
| 005 | 20250404154519.0 | ||
| 035 | |a (RuTPU)RU\TPU\network\38963 | ||
| 035 | |a RU\TPU\network\38952 | ||
| 090 | |a 667752 | ||
| 100 | |a 20220419d2021 k||y0rusy50 ba | ||
| 101 | 0 | |a eng | |
| 102 | |a CH | ||
| 135 | |a drcn ---uucaa | ||
| 181 | 0 | |a i | |
| 182 | 0 | |a b | |
| 200 | 1 | |a Pyridinone Derivatives as Interesting Formyl Peptide Receptor (FPR) Agonists for the Treatment of Rheumatoid Arthritis |f L. Crocetti, C. Vergelli, G. Guerrini [et al.] | |
| 203 | |a Text |c electronic | ||
| 300 | |a Title screen | ||
| 320 | |a [References: 35 tit.] | ||
| 330 | |a 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. | ||
| 461 | |t Molecules | ||
| 463 | |t Vol. 26, iss. 21 |v [6583, 22 p.] |d 2021 | ||
| 610 | 1 | |a труды учёных ТПУ | |
| 610 | 1 | |a электронный ресурс | |
| 610 | 1 | |a pyridinone | |
| 610 | 1 | |a formyl peptide receptors | |
| 610 | 1 | |a agonists | |
| 610 | 1 | |a rheumatoid arthritis | |
| 610 | 1 | |a molecular docking | |
| 610 | 1 | |a агонисты | |
| 610 | 1 | |a ревматоидный артрит | |
| 610 | 1 | |a лечение | |
| 610 | 1 | |a хронические заболевания | |
| 701 | 1 | |a Crocetti |b L. |g Letizia | |
| 701 | 1 | |a Vergelli |b C. |g Claudia | |
| 701 | 1 | |a Guerrini |b G. |g Gabriella | |
| 701 | 1 | |a Giovannoni |b M. P. |g Maria Paola | |
| 701 | 1 | |a Kirpotina |b L. N. |g Liliya Nikolaevna | |
| 701 | 1 | |a Khlebnikov |b A. I. |c Chemist |c Professor of Tomsk Polytechnic University |f 1963- |g Andrey Ivanovich |3 (RuTPU)RU\TPU\pers\33927 |9 17500 | |
| 701 | 1 | |a Ghelardini |b C. |g Carla | |
| 701 | 0 | |a Mannelli Lorenzo Di Cesare | |
| 701 | 1 | |a Lucarini |b E. |g Elena | |
| 701 | 1 | |a Shchepyotkin |b I. A. |g Igor Aleksandrovich | |
| 701 | 1 | |a Quinn |b M. T. |g Mark | |
| 712 | 0 | 2 | |a Национальный исследовательский Томский политехнический университет |b Инженерная школа новых производственных технологий |b Научно-образовательный центр Н. М. Кижнера |3 (RuTPU)RU\TPU\col\23556 |
| 801 | 0 | |a RU |b 63413507 |c 20220419 |g RCR | |
| 856 | 4 | |u https://doi.org/10.3390/molecules26216583 | |
| 942 | |c CF | ||