A Prodrug Approach to Improve the Physico-Chemical Properties and Decrease the Genotoxicity of Nitro Compounds

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dc.contributor.authorChin, Chung Man [UNESP]
dc.contributor.authorBosquesi, Priscila Longhin [UNESP]
dc.contributor.authordos Santos, Jean Leandro [UNESP]
dc.contributor.institutionUniversidade Estadual Paulista (Unesp)
dc.date.accessioned2014-05-20T13:24:52Z
dc.date.available2014-05-20T13:24:52Z
dc.date.issued2011-11-01
dc.description.abstractIn therapeutics research, the nitro compounds are part of an important group of drugs with multiple pharmacological activities. However, in drug design, the inclusion of a nitro group in a molecule changes the physico-chemical and electronic properties and is associated with increased mutagenicity and carcinogenicity. In addition, several studies have related the relationship between the antimicrobial and/or anti-protozoal activity and the mutagenic effect to reduction of the nitro group. This work reviews the toxicity of nitro compounds and shows how the use of prodrugs can increase the biological activity and decrease the genotoxicity of nitro compounds, without any modification in nitro reduction behavior, but rather by physico-chemical improvement. Examples are given of metronidazole and nitrofurazone prodrugs.en
dc.description.affiliationUniv São Paulo State UNESP, Sch Pharmaceut Sci, Lapdesf Lab Drug Desing, Dept Drugs & Med, BR-14802901 Araraquara, SP, Brazil
dc.description.affiliationUnespUniv São Paulo State UNESP, Sch Pharmaceut Sci, Lapdesf Lab Drug Desing, Dept Drugs & Med, BR-14802901 Araraquara, SP, Brazil
dc.description.sponsorshipFundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)
dc.description.sponsorshipConselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)
dc.description.sponsorshipPrograma de Apoio ao Desenvolvimento Científico da Faculdade de Ciências Farmacêuticas da UNESP (PADC)
dc.format.extent3515-3526
dc.identifierhttp://dx.doi.org/10.2174/138161211798194512
dc.identifier.citationCurrent Pharmaceutical Design. Sharjah: Bentham Science Publ Ltd, v. 17, n. 32, p. 3515-3526, 2011.
dc.identifier.doi10.2174/138161211798194512
dc.identifier.issn1381-6128
dc.identifier.lattes9734333607975413
dc.identifier.orcid0000-0003-4141-0455
dc.identifier.urihttp://hdl.handle.net/11449/7832
dc.identifier.wosWOS:000299637000005
dc.language.isoeng
dc.publisherBentham Science Publ Ltd
dc.relation.ispartofCurrent Pharmaceutical Design
dc.relation.ispartofjcr2.757
dc.relation.ispartofsjr0,883
dc.rights.accessRightsAcesso restrito
dc.sourceWeb of Science
dc.subjectProdrugsen
dc.subjectnitro-compoundsen
dc.subjectmetronidazolen
dc.subjectnitrofurazoneen
dc.subjectgenotoxicityen
dc.subjectphysico-chemical propertiesen
dc.titleA Prodrug Approach to Improve the Physico-Chemical Properties and Decrease the Genotoxicity of Nitro Compoundsen
dc.typeResenha
dcterms.licensehttp://www.benthamscience.com/permission.php
dcterms.rightsHolderBentham Science Publ Ltd
unesp.author.lattes9734333607975413[1]
unesp.author.orcid0000-0003-4141-0455[1]
unesp.author.orcid0000-0002-2460-2829[3]
unesp.campusUniversidade Estadual Paulista (Unesp), Faculdade de Ciências Farmacêuticas, Araraquarapt

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