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Drug Resistance Modulation in Staphylococcus Aureus, a New Biological Activity for Mesoionic Hydrochloride Compounds.doc

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Drug Resistance Modulation in Staphylococcus Aureus, a New Biological Activity for Mesoionic Hydrochloride Compounds

Molecules 2011, 16, 2023-2031; doi:10.3390/moleculeOPEN ACCESS molecules ISSN 1420-3049 /journal/molecules Article Drug Resistance Modulation in Staphylococcus Aureus, a New Biological Activity for Mesoionic Hydrochloride Compounds Cledualdo Soares de Oliveira 1, Vivyanne dos Santos Falc?o-Silva 3, José Pinto Siqueira-Júnior 3, David Peter Harding 1, Bruno Freitas Lira 1, Jorge Gon?alo Fernandes Lorenzo 2, José Maria Barbosa-Filho 2 and Petr?nio Filgueiras de Athayde-Filho 1,* 1 Department of Chemistry, Federal University of Paraíba, 58059, Jo?o Pessoa, PB, Brazil; E-Mails: aldoscarchi@.br (C.S.D.O.); kauaii@ (D.P.H.); brunofrlira@ (B.F.L.) 2 Laboratory of Pharmaceutical Technology, Federal University of Paraíba, 58051, Jo?o Pessoa, PB, Brazil; E-Mails: jgflorenzo@ (J.G.F.L.); jbarbosa@ltf.ufpb.br (J.M.B.-F.) 3 Department of Molecular Biology, Federal University of Paraíba, 58059, Jo?o Pessoa, PB, Brazil; E-Mails: jpsiq@.br (J.P.S.-J.); vivyannefalcao@.br (V.D.S.F.-S.) * Author to whom correspondence should be addressed; E-Mail: athayde-filho@quimica.ufpb.br; Tel.: +55-83-3216-7937. Received: 25 January 2011; in revised form: 19 February 2011 / Accepted: 22 February 2011 / Published: 28 February 2011 Abstract: Two salts of the mesoionic compounds 1,4-diphenyl-5-(5-nitro-2-furanyl)-1,3,4- thiadiazolium-2-thiol chloride (MC-1) and 4-phenyl-5-(5-nitro-2-furanyl)-1,3,4- thiadiazolium-2-phenylamine chloride (MC-2) were synthesized utilizing 1,4-diphenyl- thiosemicarbazide and 5-nitro-2-furoyl chloride as starting materials. Their structures were characterized by IR, 1H-NMR, 13C-NMR and elemental analysis. These compounds were analyzed for their influence on the effectiveness of norfloxacin, tetracycline, and erythromycin (standard antibiotics) against resistant strains of Staphylococcus aureus. MC-1 and MC-2, at sub-inhibitory concentrations of 16 μg/mL, favourably modulated the antibiotic activity of tetracycline