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Search Results: 1 - 10 of 311535 matches for " Eliezer J.;Lima "
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Special Dedicated to INCT-INFAR (Editorial) [Especial dedicado ao INCT-Inofar]
Eliezer J. Barreiro,Lidia Moreira Lima
Revista Virtual de Química , 2010,
Abstract:
O renascimento de um fármaco: talidomida
Lima, Lídia Moreira;Fraga, Carlos Alberto Manssour;Barreiro, Eliezer J.;
Química Nova , 2001, DOI: 10.1590/S0100-40422001000500016
Abstract: thalidomide, first synthesized in 1953, was widely prescribed for morning sickness of pregnant women from 1957 to 1961, when it was found to be seriously teratogenic, having caused serious birth defect. nowadays, a quarter of a century later, it appears that it may be a miracle drug for such diseases as leprosy, aids, cancer and tuberculosis.
Agentes antiasmáticos modernos: antagonistas de receptores de leucotrienos cisteínicos
Lima, Lídia Moreira;Fraga, Carlos Alberto Manssour;Barreiro, Eliezer J.;
Química Nova , 2002, DOI: 10.1590/S0100-40422002000500019
Abstract: in the early 1990s numerous clinical trials with antileukotriene drugs confirmed the hypothesis that cysteinyl leukotrienes are important bronchoconstrictor agents in asthma. newly released"antiasthmatic medications include antileukotriene agents which function either by blocking the interaction of leukotrienes with receptors or by inhibiting leukotriene synthesis. representatives of cysteinyl leukotriene receptors antagonists are zafirlukast (7), montelukast (8) and pranlukast (9). the bronchodilator efficacy and antiinflammatory property of antileukotriene drugs provided the main impetus behind their introduction as the first novel class of asthma therapy in more than 20 years.
Esquizofrenia: quarenta anos da hipótese dopaminérgica sob a ótica da Química Medicinal
Menegatti Ricardo,Fraga Carlos Alberto Manssour,Barreiro Eliezer J.,Lima Vera Lucia Eifler
Química Nova , 2004,
Abstract: Schizophrenia is a devastating psychiatric illness that affects 1-2% of the world population and continues as a challenge to neuroscience. In this work, we describe an account about the historical evolution of the dopaminergic hypothesis of schizophrenia discussing, from the medicinal chemistry point of view all different classes of antipsychotic drugs, emphasizing the rational design, structure activity relationships (SAR) and physico-chemical properties related with its molecular mechanism of action.
O renascimento de um fármaco: talidomida
Lima Lídia Moreira,Fraga Carlos Alberto Manssour,Barreiro Eliezer J.
Química Nova , 2001,
Abstract: Thalidomide, first synthesized in 1953, was widely prescribed for morning sickness of pregnant women from 1957 to 1961, when it was found to be seriously teratogenic, having caused serious birth defect. Nowadays, a quarter of a century later, it appears that it may be a miracle drug for such diseases as leprosy, AIDS, cancer and tuberculosis.
Agentes antiasmáticos modernos: antagonistas de receptores de leucotrienos cisteínicos
Lima Lídia Moreira,Fraga Carlos Alberto Manssour,Barreiro Eliezer J.
Química Nova , 2002,
Abstract: In the early 1990s numerous clinical trials with antileukotriene drugs confirmed the hypothesis that cysteinyl leukotrienes are important bronchoconstrictor agents in asthma. Newly released"antiasthmatic medications include antileukotriene agents which function either by blocking the interaction of leukotrienes with receptors or by inhibiting leukotriene synthesis. Representatives of cysteinyl leukotriene receptors antagonists are zafirlukast (7), montelukast (8) and pranlukast (9). The bronchodilator efficacy and antiinflammatory property of antileukotriene drugs provided the main impetus behind their introduction as the first novel class of asthma therapy in more than 20 years.
New antithrombotic aryl-sulfonylthiosemicarbazide derivatives synthesized from natural safrole
Lima, Lídia M.;Ormelli, Claudia B.;Fraga, Carlos A.M.;Miranda, Ana L.P.;Barreiro, Eliezer J.;
Journal of the Brazilian Chemical Society , 1999, DOI: 10.1590/S0103-50531999000500013
Abstract: as part of a research program aiming at the synthesis and pharmacological evaluation of novel lead-compounds exploring brazilian abundant natural products, we describe herein the synthesis and the antithrombotic profile of new aryl-sulfonylsemicarbazides and aryl-sulfonylthiosemicarbazides (10a-d). the new derivatives, designed with basis on the molecular hybridization concept, were prepared in good yields from natural safrole (9), isolated from sassafras oil. the anti-aggregating activity of these new derivatives (10a-d) on platelet aggregation induced by adp, collagen, arachidonic acid and u-46619, indicates an important antithrombotic profile for the 6-methyl-3,4-methylenedioxyphenyl-sulfonyl-n-phenylthiosemicarbazide derivative (10d), acting at the arachidonic acid cascade and representing a new lead-compound with antithrombotic activity.
Esquizofrenia: quarenta anos da hipótese dopaminérgica sob a ótica da Química Medicinal
Menegatti, Ricardo;Fraga, Carlos Alberto Manssour;Barreiro, Eliezer J.;Lima, Vera Lucia Eifler;Rates, Stela Maris Kuze;Dalla Costa, Teresa;
Química Nova , 2004, DOI: 10.1590/S0100-40422004000300015
Abstract: schizophrenia is a devastating psychiatric illness that affects 1-2% of the world population and continues as a challenge to neuroscience. in this work, we describe an account about the historical evolution of the dopaminergic hypothesis of schizophrenia discussing, from the medicinal chemistry point of view all different classes of antipsychotic drugs, emphasizing the rational design, structure activity relationships (sar) and physico-chemical properties related with its molecular mechanism of action.
Discovery of Novel Orally Active Anti-Inflammatory N-Phenylpyrazolyl-N-Glycinyl-Hydrazone Derivatives That Inhibit TNF-α Production
Renata B. Lacerda, Leandro L. da Silva, Cleverton K. F. de Lima, Eduardo Miguez, Ana Luisa P. Miranda, Stefan A. Laufer, Eliezer J. Barreiro, Carlos A. M. Fraga
PLOS ONE , 2012, DOI: 10.1371/journal.pone.0046925
Abstract: Herein, we describe the synthesis and pharmacological evaluation of novel N-phenylpyrazolyl-N-glycinyl-hydrazone derivatives that were designed as novel prototypes of p38 mitogen-activated protein kinase (MAPK) inhibitors. All of the novel synthesized compounds described in this study were evaluated for their in vitro capacity to inhibit tumor necrosis factor α (TNF-α production in cultured macrophages) and in vitro MAPK p38α inhibition. The two most active anti-TNF-α derivatives, (E)-2-(3-tert-butyl-1-phenyl-1H-pyrazol-5-ylamino)-N’-((4-(2-morpholinoethoxy)naphthalen-1-y?l)methylene)acetohydrazide(4a) and (E)-2-(3-tert-butyl-1-phenyl-1H-pyrazol-5-ylamino)-N’-(4-chlorobenzylid?ene)acetohydrazide(4f), were evaluated to determine their in vivo anti-hyperalgesic profiles in carrageenan-induced thermal hypernociception model in rats. Both compounds showed anti-inflammatory and antinociceptive properties comparable to SB-203580 used as a standard drug, by oral route at a dose of 100 μmol/kg. This bioprofile is correlated with the ability of NAH derivatives (4a) and (4f) suppressing TNF-α levels in vivo by 57.3 and 55.8%, respectively.
Therapeutic approaches for tumor necrosis factor inhibition
Barbosa, Maria Letícia de Castro;Fumian, Milla Machado;Miranda, Ana Luísa Palhares de;Barreiro, Eliezer J.;Lima, Lídia Moreira;
Brazilian Journal of Pharmaceutical Sciences , 2011, DOI: 10.1590/S1984-82502011000300002
Abstract: tumor necrosis factor (tnf) consists of an inflammatory cytokine essential for homeostasis and organism defense. despite its physiological relevance, both increased biosynthesis and release of tnf lead to the exacerbation of inflammatory and oxidative responses, which are related to the pathogenesis of a host of diseases of an inflammatory, autoimmune and/or infectious nature. in this context, effective therapeutic approaches for the modulation of tnf have been the focus of research efforts. approximately one million individuals worldwide have been treated with biotechnological inhibitors of this cytokine, the so-called anti-tnf biopharmaceuticals. however, given the high risk of infection and the limitations related to cost and administration routes, new therapeutic approaches aimed at biological targets that directly or indirectly modulate the production and/or activation of tnf appear promising alternatives for the discovery of new anti-inflammatory and immunomodulatory orally active drugs and are therefore discussed in this paper.
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