Síntese e atividade antiedematogênica de derivados N-triptofil-5-benzilideno-2,4-tiazolidinadiona e N-triptofil-5-benzilideno-rodanina

Góes, Alexandre José da Silva; Lima, Waldir Tavares de; Nagy, H.; Alves, A. J.; Faria, Antônio Rodolfo de; Lima, José Gildo de; Maia, Maria Bernadete de Souza

doi:10.1590/s0100-40422004000600013

Cited by 2 publications

(1 citation statement)

References 16 publications

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“…[4][5][6] Besides the anti-inflammatory activity by COX pathway, some thiazolidines have been described as peroxisome proliferator-activated receptor ligands (PPAR) which are capable of suppressing inflammatory process. 7 A 5-indol substitution on the central thiazolidinic ring and the absence of a sulfonyl moiety are the two structural features of the chemical series obtained by our group, 8 which are chemically related to the potent NSAID indomethacin as well as to the anti-diabetic PPARactivator thiazolidinones, as roziglitazone ( Figure 1).…”

Section: Introductionmentioning

confidence: 99%

Development and application of LC-UV method for the quantification of the anti-inflammatory thiazolidinone PG15 in rat plasma

Uchôa¹,

Cattani²,

Lima³

et al. 2008

J. Braz. Chem. Soc.

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Um método rápido e simples de cromatografia líquida com detecção por ultravioleta foi desenvolvido e validado para quantificação, em plasma de rato, do composto (5Z,E)-3-[2-(4-clorofenil)-2-oxoetil]-5-(1H-indol-3-ilmetileno)-tiazolidina-2,4-diona (PG15). Uma coluna em fase reversa C18 foi utilizada para separação do analito, seguida por detecção em UV a 385 nm. O método utilizou a precipitação do PG15 a partir do plasma e eluição isocrática com metanol:água (90:10, v/v). O tempo total da corrida foi 7,5 min. O método proposto foi validado e mostrou-se linear entre 62,5 e 4000 ng mL -1 . A precisão intra-e inter-dia, expressa como desvio padrão relativo, foi menor que 15 e 10%, respectivamente, para todas as concentrações investigadas. A exatidão, medida através dos controles da qualidade, ficou entre 86,1-114,9 %. A aplicabilidade do método validado foi testada no estudo farmacocinético pré-clínico do PG15.A simple and rapid liquid chromatography-ultraviolet detection (LC-UV) method has been developed and validated for quantifying (5Z,E)-3-[2-(4-chlorophenyl)-2-oxoethyl]-5-(1H-indol-3-ylmethylene)-thiazolidine-2,4-dione (PG15) in rat plasma. A C18 reversed phase column provided chromatographic separation of the analyte which was followed by UV detection at 385 nm. The method involves precipitation of PG15 from plasma and isocratic elution with methanol:water (90:10, v/v). Total elution time was 7.5 min. The proposed method was validated and showed linear correlation in the range of 62.5 to 4000 ng mL -1 . The within-and between-day precision, expressed as the relative standard error, were found to be less than 15 and 10 %, respectively, for all the concentrations investigated. The accuracy, measured using the quality control samples, was in the range of 86.1-114.9 %. The applicability of the validated method was tested in a pre-clinical pharmacokinetic study of the thiazolidinone PG15.

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Section: Introductionmentioning

confidence: 99%

Development and application of LC-UV method for the quantification of the anti-inflammatory thiazolidinone PG15 in rat plasma

Uchôa¹,

Cattani²,

Lima³

et al. 2008

J. Braz. Chem. Soc.

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Improved nonclinical pharmacokinetics and biodistribution of a new PPAR pan-agonist and COX inhibitor in nanocapsule formulation

Garcia

Oliveira

Pitta

et al. 2015

Journal of Controlled Release

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We report the in vitro release profile and comparative pharmacokinetics and biodistribution of a new peroxisome proliferator-activated receptor-γ agonist and cyclooxygenase inhibitor (Lyso-7) free or associated to poly(D,L-lactic acid) nanocapsules (NC) after intravenous administration in mice. Lyso-7 pertains to the class of insulin-sensitizing agents that shows potential beneficial effects in diabetes therapy. Monodispersed Lyso-7 NC with a mean diameter of 273 nm with high encapsulation efficiency (83%) were obtained. Lyso-7 dissolution rate was reduced (2.6-fold) upon loading in NC. The pharmacokinetic parameters were determined using a non-compartmental approach. In comparison with Lyso-7 in solution, the plasma-AUC increased 14-fold, the mean residence time 2.6-fold and the mean half-life (t1/2) 1.5-fold for Lyso-7-NC; the Lyso-7 plasma clearance, distribution volume and elimination rate were reduced 13, 10 and 1.4 fold, respectively, which indicates higher retention of encapsulated Lyso-7 in the blood compartment. Upon association with NC, organ exposure to Lyso-7 was higher in the heart (3.6-fold), lung (2.8-fold), spleen (2.3-fold), kidney (2-fold) and liver (1.8-fold) compared to Lyso-7 in solution. The analysis of whole data clearly indicates that body exposure to Lyso-7 was enhanced and the general toxicity reduced upon nanoencapsulation, allowing further evaluation of Lyso-7 in nonclinical and clinical studies.

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Síntese e atividade antiedematogênica de derivados N-triptofil-5-benzilideno-2,4-tiazolidinadiona e N-triptofil-5-benzilideno-rodanina

Cited by 2 publications

References 16 publications

Development and application of LC-UV method for the quantification of the anti-inflammatory thiazolidinone PG15 in rat plasma

Development and application of LC-UV method for the quantification of the anti-inflammatory thiazolidinone PG15 in rat plasma

Improved nonclinical pharmacokinetics and biodistribution of a new PPAR pan-agonist and COX inhibitor in nanocapsule formulation

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