Novel thalidomide analogues from diamines inhibit pro-inflammatory cytokine production and CD80 expression while enhancing IL-10.
Authors: Mazzoccoli, L.; Cardoso, S.H.; Amarante, G.W.; De Souza, M.V.N.; Domingues, R.; Machado, M.A.; Almeida, M.V.; Teixeira, H.C. Source: Biomedicine & Pharmacotherapy, v. 1, p. 1-10, 2012. Publisher: Elsevier Abstract Thalidomide is used to treat a variety of diseases including erythema nodosum leprosum, an inflammatory complication of leprosy. However, this drug has severe teratogenic activity […]
(2 S ,3 R )- tert -Butyl N -[4-( N -benzyl-4-fluorobenzenesulfonamido)-3-hydroxy-1-phenylbutan-2-yl]carbamate
Authors: Moreth, M.; De Souza, M.V.N.; Wardell, J.L.; Wardell, S.M.S.V.; Tiekink, E.R.T. Source: Acta Crystallographica. Section E, v. 68, p. 1138-1139, 2012. Publisher: International Union of Crystallography Abstract In the title molecule, C28H33FN2O5S, the mean plane about the tertiary amine group (sum of the angles subtended at the sp2-hybridized N atom = 359.7°) forms a dihedral […]
Drugs against TB: Are They Really Necessary?
Authors: De Souza, M.V.N. Source: Mycobacterial Diseases, v. 02, p. 1-1, 2012. Publisher: OMICS Publishing Group Abstract In the Twentieth Century, several outstanding breakthroughs towards cure and control of tuberculosis were finally found, saving millions of human lives. Due to these achievements in the 1960s, 1970s and 1980s, the scientific community believed that the disease […]
Tuberculose: uma abordagem geral dos principais aspectos
Authors: Nogueira, A.F.; Facchinetti, V.; De Souza, M.V.N.; Vasconcelos, T.A. Source: Revista Brasileira de Farmácia, v. 93, p. 3-9, 2012. Publisher: Associação Brasileira de Farmacêuticos (ABF) Abstract A tuberculose (TB) é uma infecção bacteriana grave, transmitida pelo ar e causada pela bactéria Mycobacterium tuberculosis. Nos últimos anos, o aparecimento de cepas multirresistentes colocou a tuberculose novamente […]
Structures of Two (E)-3-Substituted Cinnamoylbenzotriazole 1-Oxides
Authors: Howie, R. A.; De Souza, M.V.N.; Lima, C.H.S.; Wardell, J.L.; Wardell, S.M.S.V. Source: Journal of Chemical Crystallography, v. 42, p. 394-400, 2012. Publisher: Springer Abstract The molecule of (E)-3-(3-MeOC6H4CH=CHCO)-benzotriazole 1-oxide, 2, has a very near planar structure, while the 2-nitrophenyl ring is rotated out of the plane of the remaining atoms in (E)-3-(2-O2NC6H4CH=CHCO)-benzotriazole 1-oxide, 1. […]
In vitro anti-mycobacterial activity of (E)-N´-(monosubstituted-benzylidene) isonicotinohydrazide derivatives against isoniazid-resistant strains
Authors: Coelho, T.S.; Cantos, J.B.; Bispo, M.L.F.; Gonçalves, R.S.B.; Lima, C.H.S.; Da Silva, P.E.A.; De Souza, M.V.N. Source: Infectious Disease Reports, v. 4, p. 49-51, 2012. Publisher: PAGEPress Abstract A series of twenty-three N-acylhydrazones derived from isoniazid (INH 1-23) have been evaluated for their in vitro antibacterial activity against INH- susceptible strain of M. tuberculosis (RG500) […]
Structures of N -(arenecarbonyl)- N , N -dicyclohexylureas, cyclohexyl-NH C(O) N(cyclohexyl) C(O)Ar, (Ar = Ph, pyridin-3-yl and pyrazinyl)
Authors: Pinheiro, A.C.; De Souza, M.V.N.; Wardell, J.L.; Wardell, S.M.S.V. Source: Zeitschrift für Kristallographie, v. 227, p. 167-177, 2012. Publisher: De Gruyter Abstract The crystal structures of three N-(arenecarbonyl)-N,N′-dicyclohexylureas, [1: ArCO-N(cyclohexyl)-CO-NH-cyclohexyl: (R = Ph (1a), pyridin-3-yl (1c) and pyrazinyl (1e)] are reported from data collected at 120K. Comparison of the new findings with published data […]
Synthesis and Antitubercular Activity of Novel Amino Acid Derivatives
Authors: Costa, C.F.; Pinheiro, A.C.; Almeida, M.V.; Lourenço, M.C.S.; De Souza, M.V.N. Source: Chemical Biology & Drug Design (Print), v. 79, p. 216-222, 2012. Publisher:John Wiley & Sons, Inc. Abstract In this work, 17 new N-acylhydrazone derivatives of amino acids have been evaluated for their in vitro antibacterial activity against Mycobacterium tuberculosis H37Rv. The compounds 8b, […]
The Vital Importance of Sulfur for Life on Earth
Authors: De Souza, M.V.N.; Gomes, C.R.B.; Bispo, M.L.F. Source: Revista Química no Brasil, v. 6, p. 135-147, 2012. Publisher: WMF Martins Fontes Ltda. Abstract Keywords: Document Type: Review Article DOI: Publication date: 1 de Janeiro de 2012
Perspectives on the Development of Novel Potentially Active Quinolones Against Tuberculosis and Cancer
Authors: Facchinetti, V.; Gomes, C.R.B.; De Souza, M.V.N.; Vasconcelos, T.R.A. Source: Mini-Reviews in Medical Chemistry, v. 12, p. 866-874, 2012. Publisher: Bentham Science Abstract 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 […]
1-(7-Chloroquinolin-4-yl)-2-[(1H-pyrrol-2-yl)methylene]hydrazine: a potent compound against cancer
Authors: Montenegro, R.C.; Lotufo, L.V.; Moraes, M.O.; Pessoa, C.O.; Rodrigues, F.A.R.; Bispo, M.L.F.; Alcântara, C.C.; Kaiser, C.R.; De Souza, M.V.N. Source: Medicinal Chemistry Research (Print), v. 21, p. 3615-3619, 2012 Publisher: Springer Abstract Heteroaromatic derivatives (3a–f) have been synthesized and evaluated for their activity against four cancer cell lines. Among the studied compounds, 1-(7-Chloroquinolin-4-yl)-2-[(1H-pyrrol-2-yl)methylene]hydrazine (3e) […]
4-[(E)-2-(2-Chlorobenzylidene)hydrazin-1-yl]quinolin-1-ium chloride dihydrate
Authors: Tiekink, E.R.T.; Wardell, S.M.S.V.; Wardell, J.L.; Ferreira, M.L.; De Souza, M.V.N.; Kaiser, C.R. Source: Acta Crystallographica. Section E, v. 68, p. 1850-1851, 2012. Publisher: International Union of Crystallography Abstract In the title hydrated salt, C16H13ClN3+·Cl–·2H2O, a small twist is evident in the cation so that the chlorobenzene ring is not coplanar with the central hydrazinyl […]