Institute Tecnologia em Farmacos Farmanguinhos

Rio de Janeiro, Brazil

Institute Tecnologia em Farmacos Farmanguinhos

Rio de Janeiro, Brazil
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Boechat N.,Institute Tecnologia em Farmacos Farmanguinhos | Bastos M.M.,Institute Tecnologia em Farmacos Farmanguinhos
Current Topics in Medicinal Chemistry | Year: 2013

Tuberculosis is a severe infectious disease currently being treated with drugs that were developed more than 40 years ago. In recent years, the emergence of resistant Mycobacterium tuberculosis strains, as well as co-infection with the AIDS virus, has caused global concern about the evolution of the disease. Thus, the search for new drugs has become a necessity and a great challenge. Fluorine is a strategic element that is very useful in medicinal chemistry for its great influence on the biological activity of substances. This review highlights the importance of fluorinated molecules that are currently in clinical use or pre-clinical phases of development. Further, some substances in the prototype development stage are cited, which potentially represent future alternatives for the treatment of tuberculosis. © 2013 Bentham Science Publishers.


Pitaluga A.,Institute Tecnologia em Farmacos Farmanguinhos | Prado L.D.,Institute Tecnologia em Farmacos Farmanguinhos | Seiceira R.,Institute Tecnologia em Farmacos Farmanguinhos | Wardell J.L.,University of Aberdeen | Wardell S.M.S.V.,Institute Tecnologia em Farmacos Farmanguinhos
International Journal of Pharmaceutics | Year: 2010

The crystal structure of a monohydrate of (±)-mefloquinium chloride, (±)-[MEFHCl·(H2O)], has been obtained from data collected at 120K. Further details of the crystal structure of a hemihydrate, (±)-[MEFHCl·(H2O)], previously determined at room temperature, are also reported from data collected at 120K. The structural data, along with X-ray powder patterns, infrared spectra (both mid and near IR ranges) and DSC data, provide definitive evidence for the two hydrates. Further attempts to completely resolve the crystal structure of a tetragonal solvated phase failed due to the considerable disorder, involving the solvates, either water or methanol, even at 120K, however X-ray powder pattern and infrared spectral and DSC data for this phase are also reported. Comparisons of the data obtained for the hydrates in this study, with X-ray powder patterns and mid-infrared spectra of previously reported forms of (±)-mefloquinium chloride have highlighted erroneous assignments and allowed structural identification of previously and differently designated forms. © 2010 Elsevier B.V.


Facchinetti V.,Federal University of Fluminense | Facchinetti V.,Institute Tecnologia em Farmacos Farmanguinhos | Gomes C.R.B.,Institute Tecnologia em Farmacos Farmanguinhos | de Souza M.V.N.,Institute Tecnologia em Farmacos Farmanguinhos | Vasconcelos T.R.A.,Federal University of Fluminense
Mini-Reviews in Medicinal Chemistry | Year: 2012

Quinolones and its derivatives comprise an important group of heterocyclic compounds that exhibit a wide range of pharmacological properties such as antibacterial, antitumor, antiviral, anti-ischemic, antiparasitic and anxiolytic. Persistent efforts have been made over the years to develop novel congeners with superior biological activities and minimal potential for undesirable side-effects. The present review aims to highlight some recent discoveries on the development of novel quinolone-based compounds with potential antitubercular and anticancer activity. © 2012 Bentham Science Publishers.


De Souza M.V.N.,Institute Tecnologia em Farmacos Farmanguinhos | Wardell S.M.S.V.,CHEMSOL | Loureno M.C.S.,Institute Pesquisa e Clinica Evandro Chargas IPEC
Journal of Molecular Structure | Year: 2011

Thermolysis of (R*,S*)-(2-{[2,8- bis(trifluoromethyl)quinolin-4-yl](hydroxy)∼methyl}piperidin-1-ium) tetraphenylborate, (±)-erythro-mefloquinium tetraphenylborate, 3, in solution or neat, provides the oxazaborolidine derivative, diphenyl[(R *,S*)-(2,8-bis(trifluoromethyl)quinolin-4-yl)] piperidin-2-yl-methanolato-O,N]boron, 2. Crystal structures of solvates of 2 and 3 are reported. As shown by the 1H NMR spectrum, 2 undergoes a conformation equilibrium in solution. Both 2 and 3 exhibit important anti-tubercular activities as indicated by the minimum inhibitory concentrations (MIC) of 50 and 12.5 μg/ml, respectively, in in vitro assays against M. tuberculosis H37Rv ATTC 27294. © 2011 Elsevier B.V. All rights reserved.


Jordao A.K.,Federal University of Fluminense | Ferreira V.F.,Federal University of Fluminense | Cunha A.C.,Federal University of Fluminense | Wardell J.L.,Institute Tecnologia em Farmacos FarManguinhos | And 2 more authors.
CrystEngComm | Year: 2012

The presence of localised C-X⋯π [or C-X⋯π(CC)] interactions are shown to be pivotal in the crystal structures of (5-methyl-1-(4-X-arylamino)-1H-1,2,3-triazol-4-yl)methanol derivatives, X = H (1), F (2) and Cl (3). In the absence of halide (1), molecules aggregate into supramolecular chains via alternating ten-membered {⋯HOC 2N} 2 and 14-membered {⋯HN 2C 3O} 2 synthons. Molecules assemble into a three-dimensional architecture via edge-to-face C-H⋯π(arene) interactions occurring between the phenyl rings. In the presence of halide (i.e. F (2) and Cl (3) in the 4-position of the phenyl ring), two-dimensional arrays are formed by interconnected ten-membered {⋯HOC 2N} 2 (as seen in 1) and 24-membered {⋯HO⋯NC 2OH⋯N 4H} 2 hydrogen bonded synthons. The latter arrangement allows for the close approach of halide to the 1,2,3-triazole ring and the formation of C-X⋯π interactions which appear to be particularly significant in the case of Cl (3), as evidenced by systematic changes (i.e. elongation) in the geometric parameters within the five-membered ring. In this series of structures, the presence of C-X⋯π interactions is shown to moderate the supramolecular aggregation based on conventional hydrogen bonding. This journal is © The Royal Society of Chemistry 2012.


Costa T.E.M.M.,Institute Tecnologia em Farmacos Farmanguinhos | Dias A.P.M.,Federal University of Fluminense | Scheidegger E.M.D.,Instituto Oswaldo Cruz | Marin V.A.,Instituto Nacional Of Controle E Qualidade Em Saude
Ciencia e Saude Coletiva | Year: 2011

Since the commercial approve in 1996, the global area of transgenic crops has raised more than 50 times. In the last two decades, governments have been planning strategies and protocols for safety assessment of food and feed genetically modified (GM). Evaluation of food safety should be taken on a case-by-case analysis depending on the specific traits of the modified crops and the changes introduced by the genetic modification, using for this the concept of substantial equivalence. This work presents approaches for the risk assessment of GM food, as well as some problems related with the genetic construction or even with the expression of the inserted gene.


Neuenfeldt P.D.,Federal University of Pelotas | Duval A.R.,Federal University of Pelotas | Drawanz B.B.,Federal University of Pelotas | Rosales P.F.,Federal University of Pelotas | And 4 more authors.
Ultrasonics Sonochemistry | Year: 2011

An efficient multicomponent reaction of arenealdehydes, mercaptoacetic acid and piperonilamine under ultrasound irradiation to afford 2-aryl-3-(piperonylmethyl)-1,3-thiazolidin-4-ones is reported. Applying this methodology, eleven heterocycles were synthesized and isolated in good yields after short reaction times. © 2010 Elsevier B.V.


Vellasco Junior W.T.,Federal University of Fluminense | Gomes C.R.B.,Institute Tecnologia em Farmacos Farmanguinhos | Vasconcelos T.R.A.,Federal University of Fluminense
Mini-Reviews in Organic Chemistry | Year: 2011

Benzoxathiolones and its derivatives are important pharmacophores with diversified pharmacological activities like antibacterial, antimycotic, antioxidant and anti-inflammatory. These different biological applications for benzoxathiolone compounds have motivated new studies in searching novel derivatives with better activity results and also other applications in pharmaceutical industry. Owing to the importance of this system, the aim of this review is to present the main aspects of the chemistry and biological properties of 1,3-benzoxathiol-2-ones. © 2011 Bentham Science Publishers Ltd.


Facchinetti V.,Federal University of Fluminense | Facchinetti V.,Institute Tecnologia em Farmacos Farmanguinhos | da Reis R.R.,Federal University of Fluminense | Gomes C.R.B.,Institute Tecnologia em Farmacos Farmanguinhos | Vasconcelos T.R.A.,Federal University of Fluminense
Mini-Reviews in Organic Chemistry | Year: 2012

Benzothiazoles and its derivatives are an important group of heterocyclic compounds that exhibit a wide range of pharmacological properties such as antitumor, antimicrobial, antidiabetic, anticonvulsant and anti-inflammatory. These different biological applications for benzothiazole compounds have motivated new efforts in search for novel derivatives with improved biological activity and diverse applications in pharmaceutical industry. Owing to the importance of this system, the aim of this review is to highlight aspects reported on the chemistry and biological activity of benzothiazoles during the past few years (2000-2010). © 2012 Bentham Science Publishers.


Leishmania causes tegumental and visceral diseases called leishmaniasis. Disease control is possible interrupting the transmission cycle, but HIV co-infection, chemotheraphy toxicity and lack of a vaccine are paramount difficulties. So, is necessary to study new Leishmania molecules and investigate the possibility to develop rational drugs using these molecules as targets. Leishmania express many peptidases during their life, and cysteine are the most abundant protease and many inhibitors were developed but failed to kill parasites. On the other hand, inhibitors of serine proteases killed promastigotes, indicating the possibility of these enzymes to be important targets in the development of anti-Leishmania drugs.

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