Promising candidates in clinical trials against multidrug-resistant tuberculosis (MDR-TB) based on natural products
Authors: De Souza, M.V.N. Source: Fitoterapia. Edizione Farmaceutica, v. 80, p. 453-460, 2009. Publisher: Elsevier Abstract In the twenty first century the interest in new anti-tuberculosis drugs based on natural products, specially against MDR (multidrug-resistant) and XDR (extensively drug resistant) tuberculosis (TB) is growing, as indicated by the increasing number of publications in this field. […]
Synthesis and antitubercular activity of 7-chloro-4-quinolinylhydrazones derivatives
Authors: Candea, A.L.P.; Ferreira, M.L.; Pais, K.C.; Cardoso, L.N.F.; Kaiser, C.R.; Henriques, M.G.M.O.; Lourenço, M.C.S.; Bezerra, F.A.F.M.; De Souza, M.V.N. Source: Bioorganic & Medicinal Chemistry Letters, v. 19, p. 6272-6274, 2009. Publisher: Elsevier Abstract A series of twenty-one 7-chloro-4-quinolinylhydrazones (3a–u) have been synthesized and evaluated for their in vitro antibacterial activity against Mycobacterium tuberculosis H37Rv. […]
Synthesis and antitubercular activity of novel Schiff bases derived from d-mannitol
Authors: Ferreira, M.L.; Vasconcelos, T.R.A.; Carvalho, E.M.; Lourenço, M.C.S.; Wardell, S.M.S.V.; Wardell, J.L.; Ferreira, V.F.; De Souza, M.V.N. Source: Carbohydrate Research (Chicago, Ill.. Print), p. 2042-2047, 2009. Publisher: Elsevier Abstract Six Schiff base derivatives of d-mannitol, 1,6-dideoxy-1,6-bis-{[(E)-arylmethylidene]amino}-d-mannitol (6: aryl = XC6H4: X = o-, m– and p– Cl or NO2), have been synthesized and evaluated for their in vitro […]
(Pyrazinecarbonyl)hydrazone halobenzaldehydes: supramolecular arrays generated by face to face stacking of ribbons, formed from C H O interactions
Authors: Baddeley, T.C.; Howie, R.A.; Lima, C.H.S.; Kaiser, C.R.; De Souza, M.V.N.; Wardell, J.L.; Wardell, S.M.S.V. Source: Zeitschrift für Kristallographie, v. 224, p. 506-514, 2009. Publisher: De Gruyter Abstract The crystal structures of seven (pyrazinecarbonyl)hydrazone mono-halo-benzaldehyde derivatives, N2C4H3CONHN=CHC6H4X (X = F, Cl or Br) are reported. In all cases, hydrogen-bonds link the planar molecules edge […]
Antitubercular activity of a,x-diaminoalkanes, H2N(CH2)nNH2
Authors: Vergara, F.M.F.; Henriques, M.G.M.O.; Candea, A.L.P.; Wardell, J.L.; De Souza, M.V.N. Source: Bioorganic & Medicinal Chemistry Letters, v. 19, p. 4937-4938, 2009. Publisher: Elsevier Abstract A series of 11 α,ω-diaminoalkanes, (H2N(CH2)nNH2, n = 2–12) have been evaluated for their in vitro antibacterial activity against Mycobacterium tuberculosis H37Rv. Compounds, (H2N(CH2)nNH2, n = 9–12), exhibited a very good activities in […]
Assessing the persistence of the N H?N hydrogen bonding leading to supramolecular chains in molecules related to the anti-malarial drug, chloroquine
Authors: Kaiser, C.R.; Pais, K.C.; De Souza, M.V.N.; Wardell, J.L.; Wardell, S.M.S.V.; Tiekink, E.R.T. Source: CrystEngComm (Cambridge. Online), v. 11, p. 1133, 2009. Publisher: Royal Society of Chemistry Abstract Crystal packing patterns for a range of chloroquine derivatives have been investigated. For species where the amine-bound R substituent carries atoms not capable of forming significant hydrogen […]
Synthesis and in vitro antitubercular activity of a series of quinoline derivatives
Authors: De Souza, M.V.N.; Pais, K.C.; Kaiser, C.R.; Peralta, M.A.; Ferreira, M.L.; Lourenço, M.C.S. Source: Bioorganic & Medicinal Chemistry, v. 17, p. 1474-1480, 2009. Publisher: Elsevier Abstract A series of 33 quinoline derivatives have been synthesized and evaluated for their in vitro antibacterial activity against Mycobacterium tuberculosis H37Rv using the Alamar Blue susceptibility test and […]
3-[(E)-(7-Chloro-4-quinolyl)hydrazonomethyl]benzonitrile monohydrate
Authors: Ferreira, M.L.; De Souza, M.V.N.; Howie, R.A.; Tiekink, E.R.T.; Wardell, S.M.S.V.; Wardell, J.L. Source: Acta Crystallographica. Section E, v. 65, p. 3239-3240, 2009. Publisher: International Union of Crystallography Abstract The title monohydrate, C17H11ClN4·H2O, features an essentially planar organic molecule, as seen in the dihedral angle of 2.42 (8)° formed between the quinoline and benzene planes. […]
4-[(2-Chloroethyl)amino]quinolinium chloride monohydrate
Authors: Tiekink, E.R.T.; Wardell, S.M.S.V.; Wardell, J.L.; De Souza, M.V.N. Source: Acta Crystallographica. Section E, v. 65, p. 3120-3121, 2009. Publisher: International Union of Crystallography Abstract In the title salt hydrate, C11H12ClN2+·Cl–·H2O, the quinolinium core is essentially planar (r.m.s. deviation = 0.027 Å) with the chloroethyl side chain being almost orthogonal to the core [C-N-C-C torsion […]
7-Chloro-4-[(E)-(3-chlorobenzylidene)hydrazinyl]-1[lambda]4-quinolinium 3-chlorobenzoate
Authors: Howie, R.A.; Tiekink, E.R.T.; Wardell, S.M.S.V.; Wardell, J.L.; De Souza, M.V.N. Source: Acta Crystallographica. Section E, v. 65, p. 3204-3205, 2009 Publisher: International Union of Crystallography Abstract Reactions between either L-serine methyl ester hydrochloride (1), or the cbz derivative, methyl (S)-(+)-2-(benzyloxycarbonylamino)-3-hydroxypropanoate (2), and pyrazinoyl chloride (3), have been studied. Methyl (S)-(+)-2-benzyloxycarbonylamino-3-[(pyrazinecarbonyl)oxy]propionate (4), methyl (S)-(+)-3-hydroxy-2-[(pyrazine-2-carbonyl)amino]propionoate (7), […]
N-(2,6-Dimethylphenyl)-2-(2-thienyl)acetamide
Authors: Ferreira, M.L.; Tiekink, E.R.T.; Wardell, S.M.S.V.; Wardell, J.L.; De Souza, M.V.N. Source: Acta Crystallographica. Section E, v. 65, p. 3203-3203, 2009. Publisher: International Union of Crystallography Abstract The thienyl ring in the title compound, C14H15NOS, is disordered over two diagonally opposite positions, the major component having a site-occupancy factor of 0.569 (3). The molecule is […]
Produtos Naturais Inibidores da Transcriptase Reversa do Vírus HIV
Authors: Gonçalves, R.S.B.; Barreto, M.B.; Gomes, C.R.B.; De Souza, M.V.N. Source: Revista Fitos (ALANAC), v. 4, p. 87-107, 2009. Publisher: FIOCRUZ Abstract Atualmente, os fármacos disponíveis no combate ao vírus da AIDS podem ser classificados em seis categorias: (a) inibidores da transcriptase reversa análogos de nucleosídeos (ITRNs), (b) inibidores da transcriptase reversa não nucleosídeos (ITRNNs), […]
