Show simple item record

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.authorYe, Richard D.
dc.contributor.authorQuinn, Mark T.
dc.date.accessioned2017-05-12T19:21:09Z
dc.date.available2017-05-12T19:21:09Z
dc.date.issued2016-11
dc.identifier.citationVergelli, Claudia, Igor A Schepetkin, Giovanna Ciciani, Agostino Cilibrizzi, Letizia Crocetti, Maria Paola Giovannoni, Gabriella Guerrini, Antonella Iacovone, Liliya N. Kirpotina, Richard D Ye, and Mark T Quinn. "Synthesis of Five- and Six-Membered N-Phenylacetamido Substituted Heterocycles as Formyl Peptide Receptor Agonists." Drug Development Research (November 2016). DOI:https://dx.doi.org/10.1002/ddr.21370.en_US
dc.identifier.issn0272-4391
dc.identifier.urihttp://scholarworks.montana.edu/xmlui/handle/1/12842
dc.description.abstractPreclinical Research Formyl peptide receptors (FPRs) are G-protein-coupled receptors that play an important role in the regulation of inflammatory process and cellular dysfunction. In humans, three different isoforms are expressed (FPR1, FPR2, and FPR3). FPR2 appears to be directly involved in the resolution of inflammation, an active process carried out by specific pro-resolving mediators that modulate specific receptors. Previously, we identified 2-arylacetamido pyridazin-3(2H)-ones as FPR1- or FPR2-selective agonists, as well as a large number of mixed-agonists for the three isoforms. Here, we report a new series of 2-arylacetamido pyridazinones substituted at position 5 and their development as FPR agonists. We also synthesized a new series of 2-oxothiazolones bearing a 4-bromophenylacetamido fragment, which was fundamental for activity in the pyridazinone series. The compounds of most interest were 4a, a potent, mixed FPR agonist recognized by all three isotypes (FPR1 EC50  = 19 nM, FPR2 EC50  = 43 nM, FPR3 EC50  = 40 nM), and 4b, which had potent activity and a preference for FPR2 (EC50  = 13 nM). These novel compounds may represent valuable tools for studying FPR activation and signaling.en_US
dc.language.isoen_USen_US
dc.rightsThis is the peer reviewed version of the following article: Vergelli, Claudia, Igor A Schepetkin, Giovanna Ciciani, Agostino Cilibrizzi, Letizia Crocetti, Maria Paola Giovannoni, Gabriella Guerrini, Antonella Iacovone, Liliya N. Kirpotina, Richard D Ye, and Mark T Quinn. "Synthesis of Five- and Six-Membered N-Phenylacetamido Substituted Heterocycles as Formyl Peptide Receptor Agonists." Drug Development Research (November 2016). DOI:https://dx.doi.org/10.1002/ddr.21370, which has been published in final form at https://dx.doi.org/10.1002/ddr.21370. This article may be used for non-commercial purposes in accordance with Wiley Terms and Conditions for Self-Archiving.en_US
dc.titleSynthesis of Five- and Six-Membered N-Phenylacetamido Substituted Heterocycles as Formyl Peptide Receptor Agonistsen_US
dc.typeArticleen_US
mus.citation.journaltitleDrug Development Researchen_US
mus.identifier.categoryChemical & Material Sciencesen_US
mus.identifier.categoryHealth & Medical Sciencesen_US
mus.identifier.categoryLife Sciences & Earth Sciencesen_US
mus.identifier.doi10.1002/ddr.21370en_US
mus.relation.collegeCollege of Letters & Scienceen_US
mus.relation.departmentMicrobiology & Immunology.en_US
mus.relation.universityMontana State University - Bozemanen_US
mus.data.thumbpage4en_US


Files in this item

Thumbnail

This item appears in the following Collection(s)

Show simple item record