DEFAR - Departamento de Farmácia
URI permanente desta comunidadehttp://www.hml.repositorio.ufop.br/handle/123456789/530
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Resultados da Pesquisa
Item Synthesis of 4-octyl-2H-1,4-benzo-thiazin-3-ones.(2003) Guarda, Vera Lúcia de Miranda; Perrissin, Monique; Thomasson, François; Ximenes, Eulália Camelo Pessoa de Azevedo; Galdino, Suely Lins; Pitta, Ivan da Rocha; Luu-Duc, Cuong; Barbe, JacquesSynthesis, physical and analytical properties of 6-alkylacylamino-4-octyl-2H-1,4-benzo-thiazin-3-ones derivatives are described. These new compounds were prepared by acylation and/or alkylation of the amino group under phase transfer catalysis conditions. Acid hydrolysis of the alkylacylamino-2H-1,4-benzo-thiazin-3-ones afforded N-alkylamino-benzothiazin-3-ones. Some of these compounds were evaluated in vitro for possible bacteriostatic activity.Item Synthesis and microbiological activity of some 2H-1,4-benzothiazin-3-one derivatives.(2000) Guarda, Vera Lúcia de Miranda; Perrissin, Monique; Thomasson, François; Ximenes, Eulália Camelo Pessoa de Azevedo; Galdino, Suely Lins; Pitta, Ivan da Rocha; Luu-Duc, CuongThe synthesis and physicochemical properties of 4-butyl-2H-benzo[1,4]thiazin-3-one derivatives are described. These new compounds were synthesised by alkylation in 4-N position and acylation and/or alkylation of 6-NH2 by phase transfer catalysis. Acid hydrolysis of 6-alkylacylamino group yielded 6-alkylamino-4-butyl-2H-benzo[1,4]thiazin-3-ones. The antimicrobial in vitro activity was determined on five compounds.Item Crystal structure of 4-butyl-6-nitro-2H-1,4-benzothiazin-3-one, Z. Kristallogr.(2006) Simone, Carlos Alberto de; Guarda, Vera Lúcia de Miranda; Galdino, Suely Lins; Pitta, Ivan da RochaItem Improved nonclinical pharmacokinetics and biodistribution of a new PPAR pan-agonist and COX inhibitor in nanocapsule formulation.(2015) Garcia, Giani Martins; Oliveira, Liliam Teixeira; Pitta, Ivan da Rocha; Lima, Maria do Carmo Alves de; Vilela, José Mário Carneiro; Andrade, Margareth Spangler; Parra Abdalla, Dulcinéia Saes; Mosqueira, Vanessa Carla FurtadoWereport the in vitro release profile and comparative pharmacokinetics and biodistribution of a newperoxisome proliferator-activated receptor-γ agonist and cyclooxygenase inhibitor (Lyso-7) free or associated to poly(D,Llactic acid) nanocapsules (NC) after intravenous administration in mice. Lyso-7 pertains to the class of insulinsensitizing 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 noncompartmental 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 studiesItem On the application of knoevenagel condensation for the synthesis of benzylidene benzothiazine compounds and structural study.(2006) Souza, Ana Maria Alves de; Guarda, Vera Lúcia de Miranda; Leite, Lucia Fernanda Cavalcanti da Costa; Barbosa Filho, José Maria; Lima, Maria do Carmo Alves de; Galdino, Suely Lins; Pitta, Ivan da RochaThe synthesis and physico-chemical properties of new 6-acetylamino or 6-benzoyl-amino 2-benzylidene-4-methyl-4Hbenzo[1,4]thiazin-3-ones and 6-benzoylamino or 6-nitro 2-benzylidene-4H-benzo[1,4]thiazin-3-ones are described. These benzylidene benzothiazine compounds were prepared by the Knoevenagel condensation with benzaldehydes. The configurations and conformations of benzylidene benzothiazine derivatives were optimised using the semi-empirical method AM1.