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dc.contributor.authorVergelli, Claudia
dc.contributor.authorSchepetkin, Igor A.
dc.contributor.authorCiciani, Giovanna
dc.contributor.authorCilibrizzi, Agostino
dc.contributor.authorCrocetti, Letizia
dc.contributor.authorGiovannoni, Maria Paola
dc.contributor.authorGuerrini, Gabriella
dc.contributor.authorIacovone, Antonella
dc.contributor.authorKirpotina, Liliya N.
dc.contributor.authorKhlebnikov, Andrei I.
dc.contributor.authorYe, Richard D.
dc.contributor.authorQuinn, Mark T.
dc.identifier.citationVergelli, Claudia, Igor A. Schepetkin, Giovanna Ciciani, Agostino Cilibrizzi, Letizia Crocetti, Maria Paola Giovannoni, Gabriella Guerrini, Antonella Iacovone, Lilya N. Kirpotina, Andrei I. Khlebnikov, Richard D. Ye, and Mark T. Quinn. "2-Arylacetamido-4-phenylamino-5-substituted pyridazinones as formyl peptide receptors agonists." Bioorganic & Medicinal Chemistry 24, no. 11 (June 2016): 2530-2543. DOI: 10.1016/j.bmc.2016.04.019.en_US
dc.description.abstractN-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 =45nM), while 13a and 27b showed a moderate preference for FPR2 (EC50 =35 and 61nM, respectively). Thus, these compounds may represent valuable tools for studying FPR activation and signaling.en_US
dc.description.sponsorshipEPSRC through a Proxomics Project Award EP/I017887/1 (A.C.), National Institutes of Health IDeA Program COBRE grant GM110732 (M.T.Q.) and grant AI033503 (R.D.Y.), an equipment grant from the M.J. Murdock Charitable Trust (M.T.Q.), a USDA National Institute of Food and Agriculture Hatch project (M.T.Q.), Montana University System Research Initiative 51040-MUSRI2015-03, and the Montana State University Agricultural Experiment Station (M.T.Q.)en_US
dc.title2-Arylacetamido-4-phenylamino-5-substituted pyridazinones as formyl peptide receptors agonistsen_US
mus.citation.journaltitleBioorganic & Medicinal Chemistryen_US
mus.identifier.categoryChemical & Material Sciencesen_US
mus.identifier.categoryHealth & Medical Sciencesen_US
mus.relation.collegeCollege of Agricultureen_US
mus.relation.collegeCollege of Letters & Scienceen_US
mus.relation.departmentMicrobiology & Immunology.en_US
mus.relation.universityMontana State University - Bozemanen_US
mus.contributor.orcidQuinn, Mark T.|0000-0001-8114-5073en_US

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