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dc.contributor.authorda Silva, Marcia-
dc.contributor.authorSouza Menezes, Carla Maria-
dc.contributor.authorFerreira, Elizabeth Igne-
dc.contributor.authorLeite, Clarice Queico Fujimura-
dc.contributor.authorSato, Daisy Nakamura-
dc.contributor.authorCorreia, Cristiane Cardoso-
dc.contributor.authorPimenta, Carolina Pereira-
dc.contributor.authorAlves Botelho, Katia Cirlene-
dc.identifier.citationChemical Biology & Drug Design. Oxford: Blackwell Publishing, v. 71, n. 2, p. 167-172, 2008.-
dc.description.abstractThe Topliss method was used to guide a synthetic path in support of drug discovery efforts toward the identification of potent antimycobacterial agents. Salicylic acid and its derivatives, p-chloro, p-methoxy, and m-chlorosalicylic acid, exemplify a series of synthetic compounds whose minimum inhibitory concentrations for a strain of Mycobacterium were determined and compared to those of the reference drug, p-aminosalicylic acid. Several physicochemical descriptors (including Hammett's sigma constant, ionization constant, dipole moment, Hansch constant, calculated partition coefficient, Sterimol-L and -B-4 and molecular volume) were considered to elucidate structure-activity relationships. Molecular electrostatic potential and molecular dipole moment maps were also calculated using the AM1 semi-empirical method. Among the new derivatives, m-chlorosalicylic acid showed the lowest minimum inhibitory concentration. The overall results suggest that both physicochemical properties and electronic features may influence the biological activity of this series of antimycobacterial agents and thus should be considered in designing new p-aminosalicylic acid analogs.en
dc.publisherBlackwell Publishing-
dc.sourceWeb of Science-
dc.subjectp-aminosalicylic aciden
dc.subjectsalicylic aciden
dc.titleTopliss method in the optimization of salicylic acid derivatives as potential antimycobacterial agentsen
dc.contributor.institutionUniversidade Estadual Paulista (UNESP)-
dc.contributor.institutionUniversidade de São Paulo (USP)-
dc.contributor.institutionInstituto Adolfo Lutz (IAL)-
dc.description.affiliationUniv Estadual Paulista, Fac Ciencias Farmaceut, BR-14801902 Araraquara, SP, Brazil-
dc.description.affiliationUniv São Paulo, Fac Ciencias Farmaceut, BR-05508970 São Paulo, SP, Brazil-
dc.description.affiliationInst Adolfo Lutz Registro, BR-14085410 Ribeirao Preto, SP, Brazil-
dc.description.affiliationUnespUniv Estadual Paulista, Fac Ciencias Farmaceut, BR-14801902 Araraquara, SP, Brazil-
dc.rights.accessRightsAcesso restrito-
dc.relation.ispartofChemical Biology & Drug Design-
Appears in Collections:Artigos, TCCs, Teses e Dissertações da Unesp

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