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| Registros recuperados: 1.286 | |
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| Radwan,Awwad Abdoh; Alanazi,Fares Kaed; Al-Agamy,Mohammed Hamed. |
| Abstract Dramatically increased occurrence of both superficial and invasive fungal infections has been observed. Candida albicans appear to be the main etiological agent of invasive fungal infections. The anti-C. albicans activity of thiosemicarbazide, 1,3,4-Thiadiazole, and 1,2,4-triazole-3(4H)-thione compounds (compounds 3-23) were investigated. The MIC values of thiadiazole and triazole derivatives 10-23 were in the range of 0.08-0.17 µmol mL-1, while that of fluconazole was 0.052 µmol mL-1. Compound 11 (5-(2-(4-chlorobenzyloxy)phenyl)-N-allyl-1,3,4-thiadiazol-2-amine) and compound 18 (5-(2-(4-chlorobenzyloxy)phenyl)-4-allyl-2H-1,2,4-triazole-3(4H)-thione) were found to be the most active compounds, with MIC values of 0.08 µmol mL-1. The newly... |
| Tipo: Info:eu-repo/semantics/article |
Palavras-chave: Anti-Candida/docking studies; Thiadiazole; Triazole. |
| Ano: 2017 |
URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502017000100614 |
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| Scotti,Luciana; Fernandes,Mariane Balerine; Muramatsu,Eric; Emereciano,Vicente de Paula; Tavares,Josean Fechine; Silva,Marcelo Sobral da; Scotti,Marcus Tullius. |
| Tissue damage due to oxidative stress is directly linked to development of many, if not all, human morbidity factors and chronic diseases. In this context, the search for dietary natural occurring molecules with antioxidant activity, such as flavonoids, has become essential. In this study, we investigated a set of 41 flavonoids (23 flavones and 18 flavonols) analyzing their structures and biological antioxidant activity. The experimental data were submitted to a QSAR (quantitative structure-activity relationships) study. NMR 13C data were used to perform a Kohonen self-organizing map study, analyzing the weight that each carbon has in the activity. Additionally, we performed MLR (multilinear regression) using GA (genetic algorithms) and molecular... |
| Tipo: Info:eu-repo/semantics/article |
Palavras-chave: Flavonoids/antioxidant activity; 13C NMR; Kohonen self-organizing map. |
| Ano: 2011 |
URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502011000200005 |
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| Abbasi,Muhammad Athar; Aziz-ur-Rehman,; Qureshi,Muhammad Zahid; Khan,Farhan Mehmood; Khan,Khalid Mohmmed; Ashraf,Muhammad; Afzal,Iftikhar. |
| This manuscript reports the synthesis of a series of N-substituted derivatives of 2-phenitidine. First, the reaction of 2-phenitidine (1) with benzene sulfonyl chloride (2) yielded N-(2-ethoxyphenyl) benzenesulfonamide (3), which further on treatment with sodium hydride and alkyl halides (4a-g) furnished into new sulfonamides (5a-g). Second, the phenitidine reacted with benzoyl chloride (6) and acetyl chloride (8) to yield the reported N-benzoyl phenitidine (7) and N-acetyl phenitidine (9), respectively. These derivatives were characterized by infrared spectroscopy, ¹H-NMR, and EI-MS, and then screened against acetylcholinesterase, butylcholinesterase, and lipoxygenase enzyme, and were found to be potent inhibitors of butyrylcholinesterase alone. |
| Tipo: Info:eu-repo/semantics/article |
Palavras-chave: 2-Phenitidine/inhibitor activity; Sulfonamides; Acetamide; Benzamide; Butyrylcholinesterase. |
| Ano: 2013 |
URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502013000100014 |
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| Massaro,Renato Ramos; Brohem,Carla Abdo; Almeida,Rebeca Leite de; Rivelli,Diogo Pineda; Miyake,Juliano Andreoli; Colquhoun,Alison; Barros,Silvia Berlanga de Moraes; Maria-Engler,Silvya Stuchi. |
| ABSTRACT Gliomas account for the majority of primary malignant brain tumors and present invasive behavior into adjacent healthy tissue. While 4-NC had previously shown to induce apoptotic cell death in a melanoma model, for the glioma model described in this paper 4-NC is cytotoxic for the cells with the induction of the autophagic pathway. Trypan blue exclusion assay showed that 4-NC was cytotoxic in a dose-dependent manner for A172 and T98G cell lines. IC10 and IC50 values were at 32 µM and 41 µM for A172 and T98G respectively. Inhibition of cell proliferation was observed by total cell counts and by cell cycle analysis by flow cytometry, with cell cycle arrest of A172 and T98G cell lines respectively in the G1/G0 and S phases of the cell cycle. 4-NC... |
| Tipo: Info:eu-repo/semantics/article |
Palavras-chave: 4-Nerolidylcatechol; Glioblastoma; Cytotoxicity; Autophagy. |
| Ano: 2017 |
URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502017000300618 |
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| Beltran-Leal,Adriana; Muñoz-Ruiz,Abraham; Esparza-Villalpando,Vicente; Castro,Yolanda; Pozos-Guillen,Amaury; Flores,Héctor. |
| The purpose of the study was to evaluate the antibacterial effect of protoporphyrin IX (PpIX) generated by the exogenous administration of 5-aminolevulinic acid or δ-ALA and activated with an argon laser over a planktonic and biofilm of Enterococcus faecalis (E. faecalis) as a pharmacological therapy alternative. A planktonic strain of E. faecalis was cultured with a solution of ∂-ALA (40 µg/mL)-thioglycolate solution for 13 min, and a biofilm of E. faecalis was cultured in a δ-ALA (80 µg/mL)-thioglycolate solution for 13 min. Then, both were irradiated with an argon laser. Finally, the antibacterial effect was evaluated by counting the CFU in planktonic form, and a LIVE/DEAD viability cell test. The production and accumulation of PpIX from exogenously... |
| Tipo: Info:eu-repo/semantics/article |
Palavras-chave: Biofilm; Photodynamic therapy; 5-aminolevulinic acid. |
| Ano: 2020 |
URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502020000100572 |
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| Olaya,María del Pilar; Vergel,Nadezdha Esperanza; López,Jose Luis; Viña,Dolores; Guerrero,Mario Francisco. |
| Parkinson’s disease is a common neurodegenerative disorder. In this study, the monoamine oxidase inhibitory activity and potential anti-parkinsonian effects of 8-propyl-6H-[1,3]dioxolo[4,5-g]chromen-6-one (FCS303), a new synthetic coumarin, were evaluated. To do this, we used the reserpine model of Parkinson’s disease, an assay of levodopa/carbidopa potentiation, the catalepsy model of haloperidol, and an in vitro assay against monoamine oxidase (MAO) activity. Additionally, lipid peroxidation and protein carbonyl group quantification was performed in mice brain homogenates previously treated with haloperidol. FCS303 inhibited monoamine oxidase B (MAO-B) with an IC50 of 5.46 ± 0.36 µM; however, there was no effect on monoamine oxidase A (MAO-A). The oral... |
| Tipo: Info:eu-repo/semantics/article |
Palavras-chave: Parkinson’s disease; Monoamine oxidase B; Coumarin; Mice; Reserpine; Levodopa; Carbidopa. |
| Ano: 2020 |
URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502020000100508 |
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| Sá,Matheus Malta de; Pasqualoto,Kerly Fernanda Mesquita; Rangel-Yagui,Carlota de Oliveira. |
| Drugs acting on the central nervous system (CNS) have to cross the blood-brain barrier (BBB) in order to perform their pharmacological actions. Passive BBB diffusion can be partially expressed by the blood/brain partition coefficient (logBB). As the experimental evaluation of logBB is time and cost consuming, theoretical methods such as quantitative structure-property relationships (QSPR) can be useful to predict logBB values. In this study, a 2D-QSPR approach was applied to a set of 28 drugs acting on the CNS, using the logBB property as biological data. The best QSPR model [n = 21, r = 0.94 (r² = 0.88), s = 0.28, and Q² = 0.82] presented three molecular descriptors: calculated n-octanol/water partition coefficient (ClogP), polar surface area (PSA), and... |
| Tipo: Info:eu-repo/semantics/article |
Palavras-chave: Two-dimensional quantitative structure-property relationships (2D-QSPR); Calculated n-octanol/water partition coefficient (ClogP); Blood-brain barrier; Benzodiazepines. |
| Ano: 2010 |
URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502010000400016 |
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| Ahsan,Farogh; Mahmood,Tarique; Usmani,Shazia; Bagga,Paramdeep; Shamim,Arshiya; Tiwari,Reshu; Verma,Neeraj; Siddiqui,Mohammed Haris. |
| Cardiovascular diseases are the main source of death and morbidity in developed and developing nations. Animal models are required to propel our understanding of the pathogenesis, increase our knowledge, disease progress, and mechanism behind cardiovascular disorder, providing new approaches focused to improve the diagnostic and the treatment of these pathological conditions and additionally to test various therapeutic ways to deal with tissue regeneration and re-establish heart working following damage. A perfect model framework ought to be reasonable, effectively controlled, reproducible, and physiologically illustrative of human disease, show cardinal signs and pathology that resembles after the human ailment and ethically stable. The decision of... |
| Tipo: Info:eu-repo/semantics/article |
Palavras-chave: Myocardial infarction; Animal model; Isoproterenol; Chemical induced; Ischeamia. |
| Ano: 2020 |
URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502020000100557 |
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| Zambrone,Flávio Ailton Duque; Corrêa,Cristiana Leslie; Amaral,Ligia Mesquita Sampaio do. |
| Abstract The aim of this study was to assess the hepatotoxicity cases described in the literature, attributed to the consumption of Herbalife(r) products, and to determine whether a causal relationship exists between the reported cases of liver injury and the use of these products. A literature search was performed on the PubMed, LILACS and PAHO databases. Seven publications reporting a total of 53 cases of hepatotoxicity linked to the use of Herbalife(r) products were retrieved. All of the studies lacked sufficient information to some degree, whether related to patients' history, concomitant use of medication and/or other compounds (including alcohol), observations on interrupted use (dechallenge), results found with markers, viral serology and... |
| Tipo: Info:eu-repo/semantics/article |
Palavras-chave: Hepatotoxicity; Herbalife(r); Herbalife products(r)/consumption/hepatotoxicity; Dietary supplements; Causality assessment. |
| Ano: 2015 |
URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502015000400785 |
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| Christ,Ana Paula; Machado,Mariana Souto; Ribas,Karla Giacomelli; Schwarzbold,Alexandre Vargas; Silva,Cristiane de Bona da; Adams,Andréa Inês Horn. |
| abstract Daptomycin (DPT) was the first lipopeptide antibiotic available for commercialization. It is active against gram-positive bacteria, including resistant strains. This work aimed to develop and validate a turbidimetric microbiologic assay to determine daptomycin in an injectable form. A 3x3 design was employed, at concentrations of 1, 2 and 4.0 µg/mL. The microorganism test used was Staphylococcus aureus ATCC 6538p, and Antibiotic Medium 3 was used as the culture medium. Method validation demonstrated that the bioassay was linear (r=0.9995), precise (RSD=2.58%), accurate (recovery 100.48± 2.11%), and robust. Degradation kinetics was also performed in an alkaline medium, indicating that daptomycin degradation follows first order kinetics under these... |
| Tipo: Info:eu-repo/semantics/article |
Palavras-chave: Daptomycin/determination; Daptomycin injection/quality control; Turbidimetric microbiological assay/quantitative analysis.. |
| Ano: 2015 |
URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502015000400775 |
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| Manfio,Maria Luisa; Agarrayua,Danielle Araújo; Machado,Jaison Carlosso; Schmidt,Cleber Alberto. |
| Ceftriaxone (CFTX) sodium is a third-generation, broad-spectrum cephalosporin that is resistant to beta-lactamases. An alternative bioassay for the assessment of the potency of this drug in pharmaceutical formulations has not been previously reported. Thus, this paper reports the development and full validation of a 3 x 3 agar diffusion bioassay using a cylinder-plate method to quantify CFTX sodium in pharmaceutical samples. The strain Staphylococcus aureus ATCC 6538P was used as the test microorganism, and the results of the proposed bioassay displayed high linearity, precision, accuracy, specificity and robustness. All potency results were statistically analyzed using an analysis of variance (ANOVA) and were found to be linear (r=0.99999) in the range of... |
| Tipo: Info:eu-repo/semantics/article |
Palavras-chave: Ceftriaxone/agar diffusion assay; Ceftriaxone/quality control; Ceftriaxone/microbiological assay; Drugs/quality control. |
| Ano: 2013 |
URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502013000400015 |
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| Lucena,Antônio Edson de Souza; Sampaio,Divaldo de Almeida; Silva,Ednaldo Rosas da; Paiva,Virgínia Florêncio de; Santiago,Ana Cláudia; Leite,Ana Cristina Lima. |
| Highly purified intravenous immunoglobulin G concentrate (IV IgG) was produced with the use of polyethylene glycol associated to a single-stage precipitation by ethanol, instead of the classic Cohn-Oncley process, which employs cold alcohol as the precipitating agent, in a three-stage process. Precipitation of crude fraction containing more than 95% of immunoglobulin G was performed by liquid chromatography with a cation exchanger, CM-Sepharose, as a stationary phase. During the process, the product was subjected to two-stage viral inactivation. The first stage was performed by the action of sodium caprylate, 30 mM at pH 5.1+/- 0.1, and the second stage was performed by the action of a solvent-detergent mixture. The finished product was formulated at 5%... |
| Tipo: Info:eu-repo/semantics/article |
Palavras-chave: Blood derivatives; Immunoglobulins; Polyethylene glycol; Ultrafiltration; Ion exchange chromatography. |
| Ano: 2010 |
URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502010000400020 |
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| Registros recuperados: 1.286 | |
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