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Search Results: 1 - 10 of 367246 matches for " Solange L. de;Pinto "
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Trypanocidal activity of isolated naphthoquinones from Tabebuia and some heterocyclic derivatives: a review from an interdisciplinary study
De Moura, Kelly C. G.;Emery, Flávio S.;Neves-Pinto, Cleverson;Pinto, Maria do Carmo F. R.;Dantas, Andrea P.;Salom?o, Kelly;Castro, Solange L. de;Pinto, Ant?nio V.;
Journal of the Brazilian Chemical Society , 2001, DOI: 10.1590/S0103-50532001000300003
Abstract: naphthoquinones isolated from the wood of trees of the families bignoniaceae and verbenaceae have been subjected to an interdisciplinary study since the seventies, when dr. benjamin gilbert, at the federal university of rio de janeiro, launched a program on the chemistry of natural products active against endemic diseases. in this paper we describe the synthesis of five naphthoimidazoles, derived from this program and their activity towards t. cruzi, the etiologic agent of chagas disease. we also review the influence of chemical structure on trypanocidal action of naphthoquinones and of derived heterocycles with imidazole, oxazole, phenoxazine, indole, dipyrane and cyclopentene rings. the overall analysis corroborates the tendency of trypanocidal activity in compounds with an imidazole or oxazole ring linked to a naphthopyrane structure. two naphthoimidazoles presented higher activities (14.5x and 34.8x) than the standard crystal violet. emphasis is given to the biodiversity of the brazilian flora as a starting point for the development of an autonomous and creative medicinal chemistry.
Química no Brasil: perspectivas e necessidades para a próxima década - Documento básico
Andrade, Jailson B. de;Pinto, Angelo C.;Cadore, Solange;Vieira, Paulo Cezar;Zucco, César;Pardini, Vera L.;Curi, Luiz Roberto Liza;
Química Nova , 2005, DOI: 10.1590/S0100-40422005000700002
Abstract: over the past years the brazilian chemical society (sbq) has been working on different projects related to the development of chemistry in brazil. after a discussion throughout the country two documents have been published in quimica nova: "mobilizing axes in chemistry" and "the chemist's education". here, we describe the initial document which was the starting point for the discussion of a new series of papers published in this special issue of quimica nova which presents an overview of the chemistry in our country and the perspectives and needs for the next decade.
The Trypanocidal Activity of Naphthoquinones: A Review
Ant?nio Ventura Pinto,Solange Lisboa de Castro
Molecules , 2009, DOI: 10.3390/molecules14114570
Abstract: Naphthoquinones are compounds present in several families of higher plants. Their molecular structures confer redox properties, and they are involved in multiple biological oxidative processes. In folk medicine, especially among Indian populations, plants containing naphthoquinones have been employed for the treatment of various diseases. The biological redox cycle of quinones can be initiated by one electron reduction leading to the formation of semiquinones, unstable intermediates that react rapidly with molecular oxygen, generating free radicals. Alternatively, the reduction by two electrons, mediated by DT-diphorase, leads to the formation of hydroquinone. Lapachol, α-lapachone and β-lapachone, which are isolated from the heartwood of trees of the Bignoniaceae family, are examples of bioactive naphthoquinones. In this review, we will discuss studies investigating the activity of these natural products and their derivatives in the context of the search for alternative drugs for Chagas disease, caused by Trypanosoma cruzi, a neglected illness that is endemic in Latin America.
A Critical Review on Chagas Disease Chemotherapy
Coura, José Rodrigues;Castro, Solange L de;
Memórias do Instituto Oswaldo Cruz , 2002, DOI: 10.1590/S0074-02762002000100001
Abstract: in this "critical review" we made a historical introduction of drugs assayed against chagas disease beginning in 1912 with the works of mayer and rocha lima up to the experimental use of nitrofurazone. in the beginning of the 70s, nifurtimox and benznidazole were introduced for clinical treatment, but results showed a great variability and there is still a controversy about their use for chronic cases. after the introduction of these nitroheterocycles only a few compounds were assayed in chagasic patients. the great advances in vector control in the south cone countries, and the demonstration of parasite in chronic patients indicated the urgency to discuss the etiologic treatment during this phase, reinforcing the need to find drugs with more efficacy and less toxicity. we also review potential targets in the parasite and present a survey about new classes of synthetic and natural compounds studied after 1992/1993, with which we intend to give to the reader a general view about experimental studies in the area of the chemotherapy of chagas disease, complementing the previous papers of brener (1979) and de castro (1993).
A Critical Review on Chagas Disease Chemotherapy
Coura José Rodrigues,Castro Solange L de
Memórias do Instituto Oswaldo Cruz , 2002,
Abstract: In this "Critical Review" we made a historical introduction of drugs assayed against Chagas disease beginning in 1912 with the works of Mayer and Rocha Lima up to the experimental use of nitrofurazone. In the beginning of the 70s, nifurtimox and benznidazole were introduced for clinical treatment, but results showed a great variability and there is still a controversy about their use for chronic cases. After the introduction of these nitroheterocycles only a few compounds were assayed in chagasic patients. The great advances in vector control in the South Cone countries, and the demonstration of parasite in chronic patients indicated the urgency to discuss the etiologic treatment during this phase, reinforcing the need to find drugs with more efficacy and less toxicity. We also review potential targets in the parasite and present a survey about new classes of synthetic and natural compounds studied after 1992/1993, with which we intend to give to the reader a general view about experimental studies in the area of the chemotherapy of Chagas disease, complementing the previous papers of Brener (1979) and De Castro (1993).
Effect of drugs on Trypanosoma cruzi and on its interaction with heart muscle cell in vitro
Castro, Solange L. de;Meirelles, Maria de Nazareth L. de;
Memórias do Instituto Oswaldo Cruz , 1987, DOI: 10.1590/S0074-02761987000200009
Abstract: megazol, nifurtimox, benznidazol and allopurinol were investigated, by light and electron μscopy, for their action on t. cruzi. both the direct effect upon amastigote and trypomastigote forms and the effect upon the interaction of heart muscle cells (hmc) with bloodstream trypomastigotes were studied. the proliferation of amastigotes in warren medium was inhibited in a dose-dependent manner by megazol, nifurtimox and benznidazol. treatment of amastigotes (25-50 μm/24 h) and trypomastigotes (25 μm/24h) led to several ultrastructural alterations in the parasites. these three drugs also had a potent effect on the treatment of infected heart muscle cells when added at the beginning of the interaction or after one or three days of infection. the interiorized parasites showed a similar pattern of ultrastructural alterations as observed by the direct effect on the amastigotes. the primary heart muscle cell culture proved to be a suitable model for the study of drugs on intracellular parasites. likewise, the amastigote proliferation in axenic medium was shown to be an adequate assay for an initial trial of drugs. these parameters seem very reliable to us for a systematic investigation of the mechanism of action of new drugs.
Mechanism of action of a nitroimidazole-thiadiazole derivate upon Trypanosoma cruzi tissue culture amastigotes
Castro, Solange L. de;Meirelles, Maria de Nazareth L.;
Memórias do Instituto Oswaldo Cruz , 1990, DOI: 10.1590/S0074-02761990000100016
Abstract: megazol (cl 64,855) a very effective drug in experimental infections by trypanosoma cruzi, and also in in vitro assays with vertebrate forms of the parasite, had its parasite, had its activity upon macromolecule biosynthesis tested using tissue culture-derived amastigote forms. megazol presented a drastic inhibition of [3h]-uridine incorporation, suggesting a selective activity upon protein synthesis. comparing the three drugs, megazol was more potent than nifurtimox and benznidazole in inhibiting protein an dna synthesis. megazol showed a 91% of inhibition of [3h]-leucine incorporation whereas nifurtimox and benznidazole, 0% and 2%, respectively. these latter two drugs inhibited the incorporation of all the precursors tested at similar levels, but the concentration of benznidazole was always three times higher, suggesting different mechanisms of action or, more probably, a greater efficiency of the 5-nitrofuran derivate in relation to the 2-nitroimidazole. so, wes conclude that the mode of action of megazol is different from the ones of nifurtimox and benznidazole and that its primary effect is associated with an impairment of protein synthesis.
Effects of high glucose concentrations on the endothelial function of the renal microcirculation of rabbits
Affonso Filipe de Souza,Cailleaux Solange,Pinto Leonardo Felipe Corrêa,Gomes Marília de Brito
Arquivos Brasileiros de Cardiologia , 2003,
Abstract: OBJECTIVE: To assess the acute effects of high glucose concentrations on vascular reactivity in the isolated non diabetic rabbit kidney. METHODS: Rabbits were anaesthetized for isolation of the kidneys. Renal arteries and veins were cannulated for perfusion with Krebs-Henselleit solution and measurement of perfusion pressure. After 3 hours of perfusion with glucose 5,5 mM (control ) and 15 mM, the circulation was submitted to sub maximal precontraction (80% of maximal response) trough continuous infusion of noradrenaline 10 mM. Vascular reactivity was then assessed trough dose-responses curves with endothelium-dependent (acetylcholine) and independent (sodium nitroprusside) vasodilators. The influence of hyperosmolarity was analyzed with perfusion with mannitol 15mM. RESULTS: A significant reduction in the endothelium-dependent vasodilation in glucose 15mM group was observed compared to that in control, but there was no difference in endothelium-independent vasodilation. After perfusion with mannitol 15 mM, a less expressive reduction in endothelium-dependent vasodilation was observed, only reaching significance in regard to the greatest dose of acetylcholine. CONCLUSION: High levels of glucose similar to those found in diabetic patients in the postprandial period can cause significant acute changes in renal vascular reactivity rabbits. In diabetic patients these effects may also occur and contribute to diabetes vascular disease.
A forma??o do Químico
Andrade, Jailson B. de;Cadore, Solange;Vieira, Paulo Cezar;Zucco, César;Pinto, Angelo C.;
Química Nova , 2004, DOI: 10.1590/S0100-40422004000200033
Abstract: training of highly qualified personnel is the most transversal axis among those identified in the document "mobilizing axes in chemistry", published by sbq, in 2002, which demands to deep the discussions, initiated in the symposium "the chemist's education", whose main objective was to discuss the repercussions of that training in the teaching and in the industrial section. after the publication of an initial paper, a couple of meetings and workshops held in rio de janeiro, in december 2003, involving the national chemist community, discussed the "the role of the graduate degrees in the chemist's education" and "the chemist's education", and confirmed the need to invest in the formation of qualified human resources in profusion and in all levels. actions to be taken were delineated. presently, the graduate programs in chemistry are showing expressive results. however, although these professionals are mostly absorbed by the academy (the absorption of the industry is less significant), only a few programs give special attention to the didactical and pedagogical training. the regional decentralization is actually a tendency in most programs, but the interaction academy-economic activities is still a challenge. it is necessary to establish with the industrial section, the highly qualified professional's profile in chemistry that the industry can absorb. the undergraduation is growing in number and quality, however still excessively concentrated in the southeast area. the national "curricula guidelines" for chemistry courses, through its flexible approach, propitiate the integral, interdisciplinary (non compartmentalized) and critical-reflexive training of the professionals as citizens and as entrepreneurs. however, deficiencies are still recognized. the evaluation system of undergraduate courses has been able to identify the most fragile modalities of courses and other indicators. it was also verified that brazilian chemistry industry absorbs minimally the highly qualif
Eixos mobilizadores em química
Andrade, Jailson B. de;Cadore, Solange;Vieira, Paulo C.;Zucco, César;Pinto, ?ngelo C.;
Química Nova , 2003, DOI: 10.1590/S0100-40422003000300025
Abstract: over the last five years there have been significant changes in higher education in brazil as well as in research funding. as a contribution to the development of science and technology, and aiming to portray chemistry today in brazil, in the context of last year′s elections for president, state governors, national congress and legislative chamber, the directors and consulting council of the brazilian chemical society, sbq, initiated in 2002 a series of activities to produce a document entitled mobilizing axes in chemistry. this discusses undergraduate and graduate teaching in chemistry, a new model for research funding, and the overall state of the art, and future perspectives. six mobilizing axes have been identified and discussed to date: 1. training of highly qualified personnel; 2. decentralization, and discouragement of institutional in-breeding; 3. stimulation of entrepreneurship and interdisciplinarity; 4. a guaranteed budget for science and technology; 5. proactive interaction of academics with economic activity; and 6. removal of institutional bottle-necks of all sorts. the brazilian chemical society hopes that the new administration will in the near future begin the task of improving the national education system and increase funding for science and technology.
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