Synthesis and in vivo antimalarial evaluation of novel hydroxyethylamine derivatives
Authors: Souza, M.C.A.; Silva, T.G.; Da Silva, M.M.; Gomes, C.R.B.; Kaiser, C.R.; Henriques, M.G.M.O.; De Souza, M.V.N. Source: Medicinal Chemistry (Hilversum), v. 8, p. 266-272, 2012. Publisher: Bentham Science Abstract A series of hydroxyethylamines has been synthesized from the reaction of (2S,3S)Boc-phenylalanine epoxide with alkyl amines in good yields and evaluated for their in vivo antimalarial […]
7-Chloro-4-[(E)-2-(2,5-dimethoxybenzylidene)hydrazin-1-yl]quinoline
Authors: De Souza, M.V.N.; Ferreira, M.L.; Wardell, S.M.S.V.; Tiekink, E.R.T.; Wardell, J.L. Source: Acta Crystallographica. Section E, v. 68, p. 1244-1245, 2012. Publisher: International Union of Crystallography Abstract In the nearly planar title compound (r.m.s. deviation for the 24 non-H atoms = 0.064 Å), C18H16ClN3O2, the conformation about the N=C bond is E. Supramolecular chains propagated […]
4-[(E)-2-(2,4-Dichlorobenzylidene)hydrazin-1-yl]quinolin-1-ium chloride monohydrate
Authors: Wardell, S.M.S.V.; Tiekink, E.R.T.; Wardell, J.L.; Ferreira, M.L.; De Souza, M.V.N. Source: Acta Crystallographica. Section E, v. 68, p. 1232-1233, 2012. Publisher: International Union of Crystallography Abstract In the title hydrated salt, C16H12Cl2N3+·Cl–·H2O, there is a small twist in the cation as seen in the torsion angle linking the benzene ring to the rest of […]
7-Chloro-4-[(E)-2-(3,4,5-trimethoxybenzylidene)hydrazin-1-yl]quinoline
Authors: Ferreira, M.L.; De Souza, M.V.N.; De Souza, M.V.N.; Wardell, S.M.S.V.; Tiekink, E.R.T.; Wardell, J.L. Source: Acta Crystallographica. Section E, v. 68, p. 1214-1215, 2012. Publisher: International Union of Crystallography Abstract In the title compound, C19H18ClN3O3, the r.m.s. deviation through the 23 non-H and non-methoxy atoms is 0.088 Å, indicating a planar molecule with the exception […]
Synthesis and Antitumoral Evaluation of Benzyl (1S)-2-[2-(monosubstituted-benzylidene)hydrazino]-1-(hydroxymethyl)-2-oxoethylcarbamate
Authors: Montenegro, R.C.; Lotufo, L.V.; Moraes, M.O.; Pessoa, C.O.; Rodrigues, F.A.R.; Pinheiro, A.C.; Nogueira, T.C.M.; De Souza, M.V.N. Source: Letters in Drug Design & Discovery, v. 9(3), p. 257-262, 2012. Publisher: Bentham Science Abstract A series of 14 N-acyl-hydrazones L-serine derivatives have been synthesized and evaluated for their in vitro antitumoral activities against four neoplastic cancer […]
Cytotoxic Activity of Polysubstituted 7-chloro-4-quinolinylhydrazone Derivatives
Authors: Montenegro, R.C.; Lotufo, L.V.; Moraes, M.O.; Pessoa, C.O.; Rodrigues, F.A.R.; Pinheiro, A.C.; Nogueira, T.C.M.; De Souza, M.V.N. Source: Letters in Drug Design & Discovery, v. 9, p. 251-256, 2012. Publisher: Bentham Science Abstract A series of fourteen polysubstituted 7-chloro-4-quinolinylhydrazone derivatives (3a-n) has been synthesized and evaluated for their activity against four cancer cell lines. Among […]
Mefloquine oxazolidine derivatives, derived from mefloquine and arenecarbaldehydes: In vitro activity including against the multidrug-resistant tuberculosis strain T113
Authors: Gonçalves, R.S.B.; Kaiser, C.R.; Lourenço, M.S.C.; Bezerra, F.A.F.M.; De Souza, M.V.N.; Wardell, J.L.; Wardell, S.M.S.V.; Henriques, M.G.M.O.; Costa, T. Source: Bioorganic & Medicinal Chemistry (Print), v. 20, p. 243-248, 2012. Publisher: Elsevier Abstract 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 […]
Synthesis and antimalarial activity of thioetherhydroxyethylsulfonamides, potential aspartyl protease inhibitors, Part 3.
Authors: Vellasco, W.T.; Guedes, G.P.; Vasconcelos, T.R.A.; Vaz, M.G.F.; De Souza, M.V.N.; Krettli, A.U.; Krettli, L.G.; Aguiar, A.C.C.; Gomes, C.R.B.; Cunico, W. Source: European Journal of Medicinal Chemistry, v. 46, p. 5688-5693, 2011. Publisher: Elsevier Abstract A series of novel thioetherhydroxyethylsulfonamide derivatives has been synthesized from the coupling of intermediates 3-amino-4-phenyl-1-thioetherazine-butan-2-oles 6,7 with arenesulfonyl chlorides […]
Synthesis, cytotoxicity, and in vitro antileishmanial activity of mono-t-butyloxycarbonyl-protected diamines.
Authors: Pinheiro, A.C.; Rocha, M.N.; Nogueira, P.M.; Nogueira, T.C.M.; Jasmim, L.F.; De Souza, M.V.N.; Soares, R.P. Source: Diagnostic Microbiology and Infectious Disease, v. 71, p. 273-278, 2011. Publisher: Elsevier Abstract Leishmania amazonensis is the etiologic agent of the cutaneous and diffuse leishmaniasis. This species is often associated with drug resistance, and the conventional treatments exhibit […]
Synthesis and Antimycobacterial Activity of Novel Amino Alcohols Containing Central Core of the Anti-HIV Drugs Lopinavir and Ritonavir
Authors: Gomes, C.R.B.; Silva, M.M.; Cardinot, D.; Santos, V.K.; Cunico, W.; Lourenço, M.C.S.; De Souza, M.V.N. Source: Chemical Biology & Drug Design (Print), Japão, v. 78, n.2, p. 1031-1034, 2011. Publisher: John Wiley & Sons, Inc. Abstract Eleven new amino alcohol derivatives have been synthesized from reactions of lopinavir intermediate and heteroaromatic aldehyde in good yields. […]
Determination of efavirenz in diluted alkaline electrolyte by cathodic adsorptive stripping voltammetry at the mercury film electrode
Authors: Castro, A.A.; De Souza, M.V.N.; Rey, N.A.; Farias, P.A.M. Source: Journal of the Brazilian Chemical Society (Impresso), v. 22, p. 1662-1668, 2011. Publisher: Brazilian Chemical Society Abstract A stripping method for the determination of the antiretroviral drug efavirenz at the submicromolar concentration levels in diluted alkaline electrolyte is described. Optimum experimental conditions were: 2.0 × […]
Structures of 4-{3-(X-phenyl)perhydro-1,3-oxazolo[3,4-a]pyridin-1-yl}-2,8-bis(trifluoromethyl)quinolines (X = H, 2-O N, 3-O N and 4-O N), derived from mefloquine
Authors: Gonçalves, R.S.B.; Kaiser, C.R.; De Souza, M.V.N.; Wardell, J.L.; Wardell, S.M.S.V.; Howie, R.A. Source: Zeitschrift für Kristallographie, v. 226, p. 793-803, 2011 Publisher: De Gruyter Abstract The crystal structures of four 4-{3-(X-phenyl)perhydro-1,3-oxazolo[3,4-a]pyridin-1-yl}-2,8-bis(trifluoro-methyl)quinolines, (2: X = H, 2-O2N, 3-O2N and 4-O2N) are reported. Differences in the conformations of the molecules are illustrated by the angles […]
