| 000 | 03510nlm1a2200517 4500 | ||
|---|---|---|---|
| 001 | 649367 | ||
| 005 | 20231030040909.0 | ||
| 035 | _a(RuTPU)RU\TPU\network\14529 | ||
| 035 | _aRU\TPU\network\9765 | ||
| 090 | _a649367 | ||
| 100 | _a20160706a2016 k y0engy50 ba | ||
| 101 | 0 | _aeng | |
| 102 | _aNL | ||
| 135 | _adrcn ---uucaa | ||
| 181 | 0 | _ai | |
| 182 | 0 | _ab | |
| 200 | 1 |
_a2-Arylacetamido-4-phenylamino-5-substituted pyridazinones as formyl peptide receptors agonists _fC. Vergelli, I. A. Schepetkin (Shchepyotkin), G. Ciciani [et al.] |
|
| 203 |
_aText _celectronic |
||
| 300 | _aTitle screen | ||
| 320 | _a[References: p. 2543 (36 tit.)] | ||
| 330 | _aN-Formyl peptide receptors (FPRs: FPR1, FPR2, and FPR3) are G protein-coupled receptors that play key roles in modulating immune cells. FPRs represent potentially important therapeutic targets for the development of drugs that could enhance endogenous anti-inflammation systems associated with various pathologies, thereby reducing the progression of inflammatory conditions. Previously, we identified 2-arylacetamide pyridazin-3(2H)-ones as FPR1- or FPR2-selective agonists, as well as a large number of FPR1/FPR2-dual agonists and several mixed-agonists for the three FPR isoforms. Here, we report a new series of 2-arylacetamido-4-aniline pyridazin-3(2H)-ones substituted in position 5 as a further development of these FPR agonists. Chemical manipulation presented in this work resulted in mixed FPR agonists 8a, 13a and 27b, which had EC50 values in nanomolar range. In particular, compound 8a showed a preference for FPR1 (EC50 = 45 nM), while 13a and 27b showed a moderate preference for FPR2 (EC50 = 35 and 61 nM, respectively). Thus, these compounds may represent valuable tools for studying FPR activation and signaling. | ||
| 333 | _aРежим доступа: по договору с организацией-держателем ресурса | ||
| 461 | _tBioorganic & Medicinal Chemistry | ||
| 463 |
_tVol. 24, Iss. 11 _v[P. 2530–2543] _d2016 |
||
| 610 | 1 | _aэлектронный ресурс | |
| 610 | 1 | _aтруды учёных ТПУ | |
| 610 | 1 | _aформил-пептиды | |
| 610 | 1 | _aрецепторы | |
| 610 | 1 | _aнейтрофилы | |
| 610 | 1 | _aагонисты | |
| 701 | 1 |
_aVergelli _bC. _gClaudia |
|
| 701 | 1 |
_aSchepetkin (Shchepyotkin) _bI. A. _cdoctor-biophysicist _cleading researcher of Tomsk Polytechnic University, candidate of medical science _f1962- _gIgor Aleksandrovich _2stltpush _3(RuTPU)RU\TPU\pers\37358 |
|
| 701 | 1 |
_aCiciani _bG. _gGiovanna |
|
| 701 | 1 |
_aCilibrizzi _bA. _gAgostino |
|
| 701 | 1 |
_aCrocetti _bL. _gLetizia |
|
| 701 | 1 |
_aGiovannoni _bM. P. _gMaria Paola |
|
| 701 | 1 |
_aGuerrini _bG. _gGabriella |
|
| 701 | 1 |
_aIacovone _bA. _gAntonella |
|
| 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 |
_aYe _bR. D. _gRichard |
|
| 701 | 1 |
_aQuinn _bM. T. _gMark |
|
| 712 | 0 | 2 |
_aНациональный исследовательский Томский политехнический университет (ТПУ) _bИнститут физики высоких технологий (ИФВТ) _bКафедра биотехнологии и органической химии (БИОХ) _h6810 _2stltpush _3(RuTPU)RU\TPU\col\18693 |
| 801 | 2 |
_aRU _b63413507 _c20201103 _gRCR |
|
| 856 | 4 | _uhttp://dx.doi.org/10.1016/j.bmc.2016.04.019 | |
| 942 | _cCF | ||