Preclinical pharmacokinetic study of a new thiazolyl hydrazone derivative with antifungal activity in mice plasma by LC-MS/MS

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dc.creatorIara Rinco Silva
dc.creatorAlysson Vinícius Braga
dc.creatorMaria Beatriz de Abreu Glória
dc.creatorRenes de Resende Machado
dc.creatorIsabela Costa César
dc.creatorRenata Barbosa de Oliveira
dc.date.accessioned2022-05-20T19:01:58Z
dc.date.accessioned2025-09-09T00:44:11Z
dc.date.available2022-05-20T19:01:58Z
dc.date.issued2020-07-15
dc.description.sponsorshipCNPq - Conselho Nacional de Desenvolvimento Científico e Tecnológico
dc.description.sponsorshipFAPEMIG - Fundação de Amparo à Pesquisa do Estado de Minas Gerais
dc.description.sponsorshipCAPES - Coordenação de Aperfeiçoamento de Pessoal de Nível Superior
dc.identifier.doi10.1016/j.jchromb.2020.122180
dc.identifier.issn1570-0232
dc.identifier.urihttps://hdl.handle.net/1843/41860
dc.languageeng
dc.publisherUniversidade Federal de Minas Gerais
dc.relation.ispartofJournal of Chromatography B
dc.rightsAcesso Restrito
dc.subjectAntifúngico
dc.subjectCromatografia líquida
dc.subjectEspectrometria de massas
dc.subjectFarmacocinética
dc.subjectCamundongos
dc.subject.otherAntifungal
dc.subject.otherLiquid chromatography–tandem mass spectrometry
dc.subject.otherPharmacokinetic
dc.subject.otherRN104
dc.titlePreclinical pharmacokinetic study of a new thiazolyl hydrazone derivative with antifungal activity in mice plasma by LC-MS/MS
dc.typeArtigo de periódico
local.citation.epage7
local.citation.spage1
local.citation.volume1149
local.description.resumoRN104, named 2-[2-(cyclohexylmethylene)hydrazinyl)]-4-phenylthiazole, is a thiazolyl hydrazone derivative with promising antifungal activity. Pharmacokinetic profile of the RN104 was evaluated in mice plasma using a developed and validated bioanalytical method by LC-MS/MS. Clotrimazole was used as internal standard. The analytes were extracted by a protein precipitation procedure and separated on a C18 end-capped column and mobile phase composed of acetonitrile - 0.1% formic acid (85:15, v/v), in isocratic mode. Electrospray ionization in positive ionization mode (ESI + ) and multiple reaction monitoring (MRM) were employed using the transitions m/z 286.1 → m/z 176.1 (quantifier) and m/z 286.1 → m/z 112.2 (qualifier) for RN104 and m/z 345.2 → m/z 277.1 (quantifier) and m/z 345.2 → m/z 165.2 (qualifier) for internal standard. The method was validated and proved to be linear, accurate, precise, and selective over the range 0.625 to 40.0 ng/mL. The pharmacokinetic model that best fit the data was the bicompartmental model. The maximum plasmatic concentration was reached 20 min after administration (per os and intraperitoneal) and the highest plasma concentration of RN104 was found after per os administration at a dosage of 50 mg/kg compared to i.p. administration at 10 mg/kg.
local.publisher.countryBrasil
local.publisher.departmentFAR - DEPARTAMENTO DE ALIMENTOS
local.publisher.departmentFAR - DEPARTAMENTO DE PRODUTOS FARMACÊUTICOS
local.publisher.departmentICX - DEPARTAMENTO DE QUÍMICA
local.publisher.initialsUFMG
local.url.externahttps://www.sciencedirect.com/science/article/pii/S1570023220303809?via%3Dihub

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