Crystal structures of three 4-[3-(XC6H4)-hexahydro[1,3] oxazolo[3,4-a]pyridin-1-yl]-2,8-bis(trifluoromethyl)quinolines (X = 3-MeO, 4-MeO and 4-HO)

Authors: De Souza, M.V.N.; Gonçalves, R.S.B.; Wardell, S.M.S.V.; Wardell, J.L. Source: Zeitschrift für Kristallographie, v. 228, p. 359-368, 2013 Publisher: De Gruyter Abstract The crystal structures of three racemic 4-{3- (X-phenyl)hexahydro[1,3]oxazolo[3,4-a]pyridin-1-yl}-2,8- bis (trifluoromethyl)quinolines, 2, namely (2: X = 3-MeO, 4-MeO and 4-HO), prepared from mefloquine and XC6H5CHO, are reported. All three molecules were previously reported to […]

The Relevance of New Drug Combinations for Modern Tuberculosis Treatment – A Patent Perspective.

Authors: Pinheiro, A.C.; De Souza, M.V.N Source: Recent Patent Reviews on Anti-Infective Drug Discovery, v. 8, p. 130-138, 2013 Publisher: Bentham Science Abstract 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 […]

Comparison of the structure of ( )-2-(2-benzylidenehydrazinylidene)quinoxaline with those of its chloro- and bromobenzylidene analogues

Authors: Gomes, L.R.; Low, J.N.; Rodrigues, A.S.M.C.; Wardell, J.L.; De Souza, M.V.N.; Nogueira, T.C.M.; Pinheiro, A.C. Source: Acta Crystallographica. Section C, Crystal Structure Communications, v. 69, p. 920-926, 2013 Publisher: International Union of Crystallography (IUCr) Abstract (E)-2-(2-Benzylidenehydrazinylidene)quin­oxaline, C15H12N4, crystallized with two molecules in the asymmetric unit. The structures of six halogen derivatives of this compound were […]

7-chloro-4-quinolinylhydrazones: a promising and potent class of antileishmanial compounds.

Authors: Coimbra, E.S. ; Antinarelli, L.M.R. ; Da Silva, A.D. ; Bispo, M.L.F. ; Kaiser, C.R. ; De Souza, M.V.N. Source: Chemical Biology & Drug Design (Print), v. 81, p. 658-665, 2013. Publisher: John Wiley & Sons, Inc. Abstract 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 […]

Structures of a co-crystal of tautomers of ( )-N-7-chloro-4-(2-methoxycinnamolyhydrazinyl)quinoline and a single tautomer of the 4-methoxy analogue.

Authors:  De Souza, M.V.N.; Bispo, M.L.F. ; Alcântara, C.C.; Wardell, S.M.S.V.; Wardell, J.L. Source: Zeitschrift für Kristallographie, v. 228, p. 232-239, 2013. Publisher: De Gruyter Abstract A crystal structure determination confirmed that the product from 7-chloroquinilin-4-ylhydrazine and 4-methoxycinnanamic acid had been isolated from MeOCH2CH2OH solution as [(E)-N′-7-chloro-4-(4-methoxycinnamolyhydrazinyl)quinoline, 1. In contrast, recrystallization of the 2-MeO derivative, 2, from […]

Five -N'-benzylidene-N-methylpyrazine-2-carbohydrazides

Authors: Gomes, L.R.; Low, J.N.; Rodrigues, A.S.M.C. ; Wardell, J.L. ; Lima, C.H.S. ; De Souza, M.V.N. Source: Acta Crystallographica. Section C, Crystal Structure Communications, v. 69, p. 549-555, 2013 Publisher: International Union of Crystallography (IUCr) Abstract The compounds N‘-benzyl­idene-N-methyl­pyrazine-2-carbohydrazide, C13H12N4O, (IIa), N‘-(2-meth­oxy­benzyl­idene)-N-methyl­pyrazine-2-carbohydrazide, C14H14N4O2, (IIb), N‘-(4-cyano­benzyl­idene)-N-methyl­pyrazine-2-carbohydrazide dihydrate, C14H11N5O·2H2O, (IIc), N-methyl-N‘-(2-nitro­benzyl­idene)­pyrazine-2-carbohydrazide, C13H11N5O3, (IId), and N-methyl-N‘-(4-nitro­benzyl­idene)­pyrazine-2-carbohydrazide, C13H11N5O3, (IIe), have dihedral angles […]

Three 2-(methysulfanyl)nicotinamides

Authors: Gomes, L.R.; Low, J.N.; Wardell, J.L.; Pinheiro, A.C.; Nogueira, T.C.M.; De Souza, M.V.N. Source: Acta Crystallographica. Section C, Crystal Structure Communications, v. 69, p. 293-298, 2013 Publisher: International Union of Crystallography (IUCr) Abstract The mol­ecular conformations of three N-alkyl-2-(methyl­sulfan­yl)nicotinamide derivatives, namely N-cyclo­hexyl-2-(methyl­sulfan­yl)nicotinamide, C13H18N2OS, (I), N-isopropyl-2-(methyl­sulfan­yl)nicotinamide, C10H14N2OS, (II), in which there are two mol­ecules in the […]

Substituted 4-alkoxy-7-Cl-quinolines exhibiting π π stacking

Authors: Gomes, L.R.; Low, J.N.; Wardell, J.L.; Cardoso, L.N.F.; De Souza, M.V.N. Source: Acta Crystallographica. Section C, Crystal Structure Communications, v. 69, p. 191-194, 2013 Publisher: International Union of Crystallography (IUCr) Abstract The mol­ecules of 4-all­yloxy-7-chloro­quinoline, C12H10ClNO, (I), 7-chloro-4-meth­oxy­quinoline, C10H8ClNO, (II), and 7-chloro-4-eth­oxy­quinoline, C11H10ClNO, (III), are all planar. In all three structures, – inter­actions between the […]

A new synthesis of chiral oxazolidinones from the amino acid L-serine

Authors: Nogueira, T.C.M.; Pinheiro, A.C.; Kaiser, C.R.; Wardell, J.L.; Wardell, S.M.S.V.; De Souza, M.V.N. Source: Letters in Organic Chemistry, v. 10, p. 1-2, 2013. Publisher: Bentham Science   Abstract Cyclization of the (4S)-PhCH2OCONHCH(CH2OH)CONHN=CH-aryl, obtained in 4 steps from L-serine, on treatment with MeI and potassium carbonate, generates the chiral oxazolidinones, (4S)-N’-[(E)-(phenyl)methylidene]-Nmethyl- 2-oxo-1,3-oxazolidine-4-carbohydrazides. Overall the formation of […]

Synthesis and Antitubercular Evaluation of N -Arylpyrazine and N,N -Alkyl-diylpyrazine-2-carboxamide Derivatives

Authors: Bispo, M.L.F.; Gonçalves, R.S.B.; Lima, C.H.S.; Cardoso, L.N.F.; Lourenço, M.C.S.; DE Souza, M.V.N. Source: Journal of Heterocyclic Chemistry, v. 49, p. 1317-1322, 2012. Publisher: John Wiley & Sons, Inc. Abstract Two series of pyrazinamide (PZA) derivatives have been synthesized and evaluated for their in vitro antibacterial activity against Mycobacterium tuberculosis H37Rv. Some compounds exhibited […]

Simultaneous analysis of first-line anti-tuberculosis drugs in tablets by UV spectrophotometry compared to capillary zone electrophoresis

Authors: Marcellos, L.F.; Faria, A.F.; De Souza, M.V.N.; Almeida, M.R.; Sabin, G.P.; Poppi, R.J.; Oliveira, M.A.L. Source: Central European Journal of Chemistry, v. 10, p. 1808-1816, 2012. Publisher: De Gruyter Abstract The development and optimization of a novel UV spectrophotometric methodology was proposed for simultaneous analysis of ethambutol (ETB), isoniazid (ISO), rifampicin (RIF) and pyrazinamide (PYR), […]

Simultaneous Analysis of Isoniazid and Its Impurities by CZE

Authors: Faria, A.F.; Vasconcelos, J.P.; Gonçalves, R.S.B.; De Souza, M.V.N. Oliveira, M.A.L. Source: Chromatographia (Wiesbaden), v. 75, p. 1335-1339, 2012. Publisher: Springer Abstract An alternative methodology for simultaneous determination of isoniazid, isonicotinic acid, 4-cyanopyridine, ethyl isonicotinate and isonicotinamide by capillary zone electrophoresis, within an analysis time of 11 min, is proposed. An electrolyte composed by 50 mmol L−1 of […]