Institute Tecnologia em Farmacos Far Manguinhos

Rio de Janeiro, Brazil

Institute Tecnologia em Farmacos Far Manguinhos

Rio de Janeiro, Brazil
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PubMed | Sunway University, University of Aberdeen, CHEMSOL and Institute Tecnologia em Farmacos Far Manguinhos
Type: Journal Article | Journal: Acta crystallographica. Section E, Crystallographic communications | Year: 2016

In the title carbohydrazide, C10H7N3O4S, the dihedral angle between the terminal five-membered rings is 27.4(2), with these lying to the same side of the plane through the central CN2C(=O) atoms (r.m.s. deviation = 0.0403), leading to a curved mol-ecule. The conformation about the C=N imine bond [1.281(5)] is E, and the carbonyl O and amide H atoms are anti. In the crystal, N-HO hydrogen bonds lead to supra-molecular chains, generated by a 41 screw-axis along the c direction. A three-dimensional architecture is consolidated by thienyl-C-HO(nitro) and furanyl-C-HO(nitro) inter-actions, as well as - inter-actions between the thienyl and furanyl rings [inter-centroid distance = 3.515(2)]. These, and other, weak inter-molecular inter-actions, e.g. nitro-N-O(thien-yl), have been investigated by Hirshfeld surface analysis, which confirms the dominance of the conventional N-HO hydrogen bonding to the overall mol-ecular packing.


Rodrigues F.A.R.,Federal University of Ceará | Bomfim I.D.S.,Federal University of Ceará | Cavalcanti B.C.,Federal University of Ceará | Pessoa C.,Federal University of Ceará | And 5 more authors.
Chemical Biology and Drug Design | Year: 2014

A series of 23 racemic mefloquine-oxazolidine derivatives, 4-[3-(aryl)hexahydro[1,3]oxazolo[3,4-a]pyridin-1-yl]-2,8-bis(trifluoromethyl) quinolines, derived from (R, S)-(±)-mefloquine and arenealdehydes, have been evaluated for their activity against four cancer cell lines (HCT-8, OVCAR-8, HL-60, and SF-295). Good cytotoxicities have been determined with IC50 values ranging from 0.59 to 4.79 μg/mL. In general compounds with aryl groups having strong electron-releasing substituents, such as HO and MeO, or electron-rich heteroaryl groups, for example imidazol-2-y-l, are active. However, other factors such as steric effects may play a role. As both the active and non-active conformations of the mefloquine-oxazolidine derivatives are similar, it is concluded that molecular conformations do not play a significant role either. This study is the first to evaluate mefloquine derivatives as antitumor agents. The mefloquine-oxazolidine derivatives are considered to be useful leads for the rational design of new antitumor agents. A series of twenty three racemic mefloquine-oxazolidine derivatives have been evaluated for their activity against 3-5 cancer cell lines SF-295, HCT-116, OVCAR-8, HCT-8 and HL-60. Cytotoxicities have been determined with IC 50 values ranging from 0.59 to 4.79 μg/mL. © 2013 John Wiley & Sons A/S.


Faria A.F.,Institute Ciencias Exatas | De Souza M.V.N.,Institute Tecnologia em Farmacos Far Manguinhos | Bruns R.E.,University of Sao Paulo | De Oliveira M.A.L.,Institute Ciencias Exatas
Talanta | Year: 2010

An alternative methodology for simultaneous analysis of ethambutol, isoniazid, rifampicin and pyrazinamide in pharmaceutical formulations by capillary zone electrophoresis under UV direct detection with an analysis time of 8.0 min is proposed. Background running was based on the effective mobility curve of the analytes and an optimum separation condition was achieved using a 33 Box-Behnken design, with Brij 35, Cu2+ and acetic acid/sodium acetate buffer as factors. An electrolyte consisting of 50.0 mmol L-1 of acetic acid/sodium acetate buffer, 12.5 mmol L-1 of CuSO4, and standard and sample solutions prepared in 2.00 mmol L-1 of Brij 35 and 12.5 mmol L-1 of CuSO4 were optimized. After evaluating validation parameters, the method was successfully applied to the analysis of samples in the form of tablets and sachets. © 2010 Elsevier B.V. All rights reserved.


Pinheiro A.C.,Institute Tecnologia em Farmacos Far Manguinhos | Nogueira T.C.M.,Institute Tecnologia em Farmacos Far Manguinhos | De Souza M.V.N.,Institute Tecnologia em Farmacos Far Manguinhos | De Souza M.V.N.,Federal University of Rio de Janeiro
Anti-Cancer Agents in Medicinal Chemistry | Year: 2016

Heterocyclic compounds are a class of substances, which play a critical role in modern drug discovery being incorporated in the structure of a large variety of drugs used in many different types of diseases. Quinoxaline is an important heterocyclic nucleus with a wide spectrum of biological activities, and recently much attention has been found on anticancer drug discovery based on this class. Owing to the importance of this system, the aim of this review is to provide an update on the synthesis and anticancer activity of quinoxaline derivatives covering articles published between 2010 and 2015. © 2016 Bentham Science Publishers.


Cardoso S.H.,Federal University of Alagoas | Barreto M.B.,Federal University of Rio de Janeiro | Lourenco M.C.S.,Institute Pesquisas Clinica Evandro Chagas | Henriques M.D.G.M.D.O.,Institute Tecnologia em Farmacos Far Manguinhos | And 3 more authors.
Chemical Biology and Drug Design | Year: 2011

The present article describes a series of 21 N'-benzylidene-2-oxo-2H-chromene-3-carbohydrazides 4a-4v, which were synthesized and evaluated for their cell viabilities in non-infected and Mycobacterium bovis Bacillus Calmette-Guerin-infected macrophages. Subsequently, the non-cytotoxic compounds 4c, 4g, 4h, 4j, 4l and 4t were assessed against Mycobacterium tuberculosis ATCC 27294 using the microplate Alamar Blue assay and the activity expressed as the minimum inhibitory concentration in μg/mL. These compounds exhibited a significant activity (50-100μg/mL) when compared to the first-line drugs, such as pyrazinamide (PZA >100μg/mL). These results could be considered a good starting point for further studies to develop new lead compounds to treat multidrug-resistant tuberculosis. The present article describes a series of twenty-one coumarine derivatives, which were synthesized and evaluated against Mycobacterium tuberculosis. © 2011 John Wiley & Sons A/S.


Coimbra E.S.,Federal University of Juiz de fora | Antinarelli L.M.R.,Federal University of Juiz de fora | da Silva A.D.,Federal University of Juiz de fora | Bispo M.L.F.,Institute Tecnologia em Farmacos Far Manguinhos | And 4 more authors.
Chemical Biology and Drug Design | Year: 2013

In this work, we report the antileishmanial evaluation of twenty 7-chloro-4-quinolinyl hydrazone derivatives (1-20). Firstly, the compounds were tested against promastigotes of four different Leishmania species. After that, all derivatives were assayed against L. braziliensis amastigotes and murine macrophages. Furthermore, it was investigated whether the antiamastigote L. braziliensis effect of the compounds could be associated with nitric oxide production. Compounds 6 and 7 showed a strong leishmanicidal activity against intracellular parasite with IC50 in nanogram levels (30 and 20 ng/mL, respectively). Appreciable activity of three compounds tested can be considered an important finding for the rational design of new leads for antileishmanial compounds. © 2013 John Wiley & Sons A/S.


Goncalves R.S.B.,Institute Tecnologia em Farmacos Far Manguinhos | de Souza M.V.N.,Institute Tecnologia em Farmacos Far Manguinhos
Current Respiratory Medicine Reviews | Year: 2010

In the last three decades, an increasing number of pathogens resistant to common antibiotics have been a serious threat to public health worldwide. Pleuromutilin, its derivatives and others natural products are important in the fight against pathogen resistant to common antibiotics, such as in respiratory diseases. The aim of the current review is to highlight the most important pleuromutilin derivatives described in the literature between the years of 2007 and 2009. © 2010 Bentham Science Publishers Ltd.


Porto B.L.S.,Federal University of Juiz de fora | de Souza M.V.N.,Institute Tecnologia em Farmacos Far Manguinhos | de Oliveira M.A.L.,Federal University of Juiz de fora
Analytical Sciences | Year: 2011

Qualitative differentiation between natural and enriched chicken eggs through omega (ω) 3 fatty acid profiles by capillary zone electrophoresis (CZE) under direct UV detection at 200 nm is proposed. The electrolyte background consisted of 12.0 mmol L-1 tetraborate buffer (pH 9.2) mixed with 12.0 mmol L-1 Brij 35, 17% acetonitrile (ACN) and 33% methanol (MeOH). Omega 3 fatty acid profile in chicken egg samples were analyzed by CZE system and confirmed by single-quadrupole mass spectrometry with an electrospray ionization probe set to negative ionization mode after sample preparation by the Folch method. The results showed that ω fatty acid profiles analyzed by the CZE approach can be used to chemical markers to monitor fraud, presenting simplicity, short analysis time (10 min) and low cost as advantages. 2011 © The Japan Society for Analytical Chemistry.


Pinheiro A.C.,Institute Tecnologia em Farmacos Far Manguinhos | de Souza M.V.N.,Institute Tecnologia em Farmacos Far Manguinhos
Recent Patents on Anti-Infective Drug Discovery | Year: 2013

Drug combinations (DCs) have been successfully used in different kinds of diseases such as cancer, AIDS, malaria, infectious diseases, asthma, diarrhea, hypertension, neurological disorders, among others. In this context, an important concept in drug discovery relates to the fixed-dose combinations (FDC), which can be defined as a formulation of two or more biologically active substances, combined in a single drug, and available at certain fixed doses. FDC presents several advantages, such as reduced risks of emergence of drug resistant strains, improvement of patient compliance, reduced costs of treatment and a simplified drug supply management, shipping and distribution. Due to the importance of DCs in drug discovery, the purpose of this review is to highlight the importance of this strategy for tuberculosis treatment and also for studies of new promising drug combinations to be used against this disease, specially focused on resistant bacterial strains. Relevant patents concerning combined treatment of tuberculosis are analyzed. © 2013 Bentham Science Publishers.


Da Silva J.A.F.,University of Campinas | De Castro N.V.,University of Campinas | De Jesus D.P.,University of Campinas | Faria A.F.,Federal University of Juiz de fora | And 2 more authors.
Electrophoresis | Year: 2010

A method for the determination of ethambutol (EMB), a first-line drug against tuberculosis, based on CE with capacitively coupled contactless conductivity detection is proposed. The separation of EMB and its main product of degradation were achieved in less than 3 min with a resolution of 2.0 using a BGE composed of 50 mmol/L histidine and 30 mmol/L MES, pH 6.30. By raising the pH to 8.03, the analysis time was reduced to 1.0 min, but with a significant loss of resolution (0.7). Using the best separation conditions, linearity of 0.9976 (R2, five data points), sensitivity of 1.26 x 10-4V min μmol-1 L, and LOD and quantification of 23.5 and 78.3 μmol/L, respectively, were obtained. Recoveries at four levels of concentration ranged from 95 to 102% and the concentration range studied ranged from 100 to 500 μmol/L. The results obtained for the determination of EMB in pharmaceutical formulations were compared with those obtained by using CE with photometric detection. © 2010 Wiley-VCH Verlag GmbH & Co. KGaA.

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