Universidad Peruana Cayetano Heredia

Synthesis, antileishmanial activity and cytotoxicity of 2,3-diaryl- and 2,3,8-trisubstituted imidazo[1,2-a]pyrazines

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dc.contributor.author Marchand, Pascal
dc.contributor.author Bazin, Marc-Antoine
dc.contributor.author Pagniez, Fabrice
dc.contributor.author Riviere, Guillaume
dc.contributor.author Bodero, Lizeth
dc.contributor.author Marhadour, Sophie
dc.contributor.author Nourrisson, Marie-Renee
dc.contributor.author Picot, Carine
dc.contributor.author Ruchaud, Sandrine
dc.contributor.author Bach, Stephane
dc.contributor.author Baratte, Blandine
dc.contributor.author Sauvain, Michel Henri Auguste
dc.contributor.author Pareja, Denis Castillo
dc.contributor.author Vaisberg Wollach, Abraham Jaime
dc.contributor.author Le Pape, Patrice
dc.date.accessioned 2019-02-06T14:52:34Z
dc.date.available 2019-02-06T14:52:34Z
dc.date.issued 2015
dc.identifier.uri https://hdl.handle.net/20.500.12866/5310
dc.description.abstract A series of original 2-phenyl-3-(pyridin-4-yl)imidazo[1,2-a]pyrazines and the 3-iodo precursors, bearing a polar moiety at the C-8 position, was synthesized and evaluated for their antileishmanial activities. Two derivatives exhibited very good activity against the promastigote and the amastigote forms of Leishmania major in the micromolar to submicromolar ranges, coupled with a low cytotoxicity against macrophages and 3T3 mouse fibroblast cells. Through LmCK1 inhibition assay, investigations of the putative molecular target of these promising antileishmanial compounds will be discussed. en_US
dc.language.iso eng
dc.publisher Elsevier
dc.relation.ispartofseries European Journal of Medicinal Chemistry
dc.rights info:eu-repo/semantics/restrictedAccess
dc.rights.uri https://creativecommons.org/licenses/by-nc-nd/4.0/deed.es
dc.subject Humans en_US
dc.subject Animals en_US
dc.subject Molecular Structure en_US
dc.subject Mice en_US
dc.subject Dose-Response Relationship, Drug en_US
dc.subject Fibroblasts/drug effects en_US
dc.subject Mice, Inbred BALB C en_US
dc.subject Cell Line en_US
dc.subject Antileishmanial activity en_US
dc.subject Antiprotozoal Agents/chemical synthesis/chemistry/pharmacology en_US
dc.subject Casein kinase 1 en_US
dc.subject Cell Proliferation/drug effects en_US
dc.subject Direct arylation en_US
dc.subject Imidazo[1,2-a]pyrazines en_US
dc.subject Imidazoles/chemical synthesis/chemistry/pharmacology en_US
dc.subject Leishmania major/drug effects en_US
dc.subject Macrophages/drug effects en_US
dc.subject Pyrazines/chemical synthesis/chemistry/pharmacology en_US
dc.subject Structure-Activity Relationship en_US
dc.title Synthesis, antileishmanial activity and cytotoxicity of 2,3-diaryl- and 2,3,8-trisubstituted imidazo[1,2-a]pyrazines en_US
dc.type info:eu-repo/semantics/article
dc.identifier.doi https://doi.org/10.1016/j.ejmech.2015.09.002
dc.subject.ocde https://purl.org/pe-repo/ocde/ford#3.01.06
dc.relation.issn 1768-3254


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