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Goncalves R.S.B.,Institute Tecnologia em Farmacos Far Manguinhos | Goncalves R.S.B.,Federal University of Rio de Janeiro | Kaiser C.R.,Federal University of Rio de Janeiro | Loureno M.C.S.,Institute Pesquisas Clinica Evandro Chagas IPEC | And 4 more authors.
European Journal of Medicinal Chemistry | Year: 2010

In this work, we report the synthesis and the antitubercular evaluation of 16 new mefloquine derivatives, formed from reactions between mefloquine and benzaldehydes, with the activity expressed as the minimum inhibitory concentration (MIC) in μM. The compounds were non-cytotoxic and exhibited an important activity (12.6 μM). The appreciable activity of these compounds can be considered an important finding for the rational design of new leads for anti-TB compounds. © 2010 Elsevier Masson SAS. All rights reserved.


Gonalves R.S.B.,Institute Tecnologia em Farmacos Far Manguinhos | Gonalves R.S.B.,Federal University of Rio de Janeiro | Kaiser C.R.,Federal University of Rio de Janeiro | Loureno M.C.S.,Institute Pesquisas Clinica Evandro Chagas IPEC | And 6 more authors.
Bioorganic and Medicinal Chemistry | Year: 2012

Ten new mefloquine-oxazolidine derivatives, 4-[(1S,8aR)-3-(aryl) hexahydro[1,3]oxazolo[3,4-a]pyridin-1-yl]-2,8-bis(trifluoromethyl)quinoline (1: aryl = substituted phenyl) and 4-[(1S,8aR)-3-(heteroaryl)hexahydro[1,3] oxazolo[3,4-a]pyridin-1-yl]-2,8-bis(trifluoromethyl)quinoline [2: heteroaryl = 5-nitrothien-2-yl (2a); 5-nitrofuran-2-yl (2b) and 4H-imidazol-2-yl) (2c)], have been synthesized and evaluated against Mycobacterium tuberculosis. Compounds 1f (aryl = 3-ethoxyphenyl), 1g (Ar = 3,4,5-(MeO) 3-C 6H 2) and 2c were slightly more active than mefloquine (MIC = 33 μM) with MICs = 24.5, 22.5 and 27.4, respectively, whereas compounds 1e (aryl = 3,4-(MeO) 2-C 6H 3) and 2a (MICs = 11.9 and 12.1 μM, respectively) were ca. 2.7 times more active than mefloquine, with a better tuberculostatic activity than the first line tuberculostatic agent ethambutol (MIC = 15.9). The compounds were also assayed against the MDR strain T113 and the same MICs were observed. Thus the new derivatives have advantages over such anti-TB drugs as isoniazid, rifampicin, ethambutol and ofloxacin, for which this strain is resistant. The most active compounds were not cytotoxic to Murine Macrophages Cells in a concentration near their MIC values. © 2011 Elsevier Ltd. All rights reserved.


Bispo M.D.L.F.,Institute Tecnologia em Farmacos Far Manguinhos | Goncalves R.S.B.,Institute Tecnologia em Farmacos Far Manguinhos | Lima C.H.D.S.,Institute Tecnologia em Farmacos Far Manguinhos | Cardoso L.N.D.F.,Institute Tecnologia em Farmacos Far Manguinhos | And 2 more authors.
Journal of Heterocyclic Chemistry | Year: 2012

Two series of pyrazinamide (PZA) derivatives have been synthesized and evaluated for their in vitro antibacterial activity against Mycobacterium tuberculosis H37Rv. Some compounds exhibited minimum inhibitory concentration activity of 50-100 μg/mL, greater than the first line antituberculosis drug PZA in Alamar Blue assay (>100 μg/mL). The obtained activities can be considered promising results, which characterizes these compounds as good start points to development of new antitubercular agents. © 2012 HeteroCorporation.


Carvalho S.A.,Institute Tecnologia em Farmacos Farmanguinhos | Carvalho S.A.,Federal University of Rio de Janeiro | da Silva E.F.,Institute Tecnologia em Farmacos Farmanguinhos | Lourenco M.C.S.,Institute Pesquisas Clinica Evandro Chagas IPEC | And 2 more authors.
Letters in Drug Design and Discovery | Year: 2010

In this work we report the tuberculostatic profile of a series of 5-phenyl-1,3,4-thiadiazole-2-arylhydrazone derivatives (1a-m). The evaluation of their in vitro antibacterial activity against Mycobacterium tuberculosis H37Rv was expressed as the minimum inhibitory concentration (MIC) in μg/mL. The compounds 1g and 1h exhibited inhibitory activity of 6.25 μg/mL and 1.25 μg/mL respectively, and can be considered as a good start point for the discovery of new lead compounds in the field of multi-drug resistant tuberculosis. © 2010 Bentham Science Publishers Ltd.


Ferreira M.D.L.,Institute Tecnologia em Farmacos Far Manguinhos | Ferreira M.D.L.,Federal University of Rio de Janeiro | Goncalves R.S.B.,Institute Tecnologia em Farmacos Far Manguinhos | Goncalves R.S.B.,Federal University of Rio de Janeiro | And 7 more authors.
TheScientificWorldJournal | Year: 2010

Two series of N′-(E)-heteroaromatic-isonicotinohydrazide derivatives (3a-f and 4a-b) and 1-(7-chloroquinolin-4-yl)-2-[(heteroaromatic)methylene] hydrazone derivatives (5a-f and 6a-b) have been synthesized and evaluated for their in vitro antibacterial activity against Mycobacterium tuberculosis H 37Rv. Several compounds were noncytotoxic and exhibited significant minimum inhibitory concentration (MIC) activity (3.12, 2.50, 1.25, or 0.60 μg/mL), which can be compared to that of the first-line drugs ethambutol (3.12 μg/mL) and rifampicin (2.0 μg/ml). These results can be considered an important starting point for the rational design of new leads for anti-TB compounds. ©2010 with author.

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