Anticholinesterasic, Nematostatic and Anthelmintic Activities of Pyridinic and Pyrazinic Compounds

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dc.contributor.authorValli, M. [UNESP]
dc.contributor.authorDanuello, A. [UNESP]
dc.contributor.authorPivatto, M. [UNESP]
dc.contributor.authorSaldana, J. C.
dc.contributor.authorHeinzen, H.
dc.contributor.authorDominguez, L.
dc.contributor.authorCampos, V. P.
dc.contributor.authorMarqui, S. R. [UNESP]
dc.contributor.authorYoung, M. C. M.
dc.contributor.authorViegas, C.
dc.contributor.authorSilva, D. H. S. [UNESP]
dc.contributor.authorBolzani, Vanderlan da Silva [UNESP]
dc.contributor.institutionUniversidade Estadual Paulista (Unesp)
dc.contributor.institutionUniv Republica
dc.contributor.institutionUniversidade Federal de Lavras (UFLA)
dc.contributor.institutionIBt Inst Bot
dc.contributor.institutionUniversidade Federal de Alfenas (UNIFAL)
dc.date.accessioned2014-05-20T14:20:12Z
dc.date.available2014-05-20T14:20:12Z
dc.date.issued2011-08-01
dc.description.abstractIn the search for acetylcholinesterase inhibitors as a potential target for the discovery of anthelmintic drugs, a series of 27 pyridinic and pyrazinic compounds have been designed on the basis of molecular hybridization of two known AChE inhibitors, namely, tacrine and (-)-3-O-acetylspectaline, and on the concept of isosterism. The synthesized compounds generally presented moderate anticholinesterasic activities when compared with the positive control physostigmine, but one compound (ethyl 2-[(6-chloropyrazin-2-yl) sulfanyl] acetate, 11) exhibited an in vitro ability to immobilize the root-knot nematode Meloidogyne incognita that was highly comparable to that of the positive control Temik. Moreover, in anthelmintic assays against the gastrointestinal parasitic nematode Nippostrongylus brasiliensis (L4), some of the compounds, such as (6-chloropyrazin-2-yl) sulfanyl ethanol (32, EC(50) = 33 nM), presented activities that were considerably stronger than that of the positive control albendazole (EC(50) = 340 nM). In the light of the positive results obtained in the anthelmintic evaluations, the acute oral toxicity of the representative compound diethyl 2,2'-[(3-nitropyridine-2,6-diyl) bissulfanediyl] diacetate (7) was determined in rats, and the drug was shown to be non-toxic at a dose of 2000 mg/kg. These results, allied with the relatively simple structures of the active compounds and their facile synthesis, highlight their potential use as anthelmintic or nematicidic agents.en
dc.description.affiliationUNESP Univ Estadual Paulista, Dept Quim, Nucleo Bioensaios Biossintese & Ecofisiol Prod Na, Inst Quim, BR-14801970 Araraquara, SP, Brazil
dc.description.affiliationUniv Republica, Fac Quim, Montevideo, Uruguay
dc.description.affiliationUFLA Universidade Federal de Lavras (UFLA), Dept Fitopatol, BR-37200000 Lavras, MG, Brazil
dc.description.affiliationIBt Inst Bot, Secao Fisiol & Bioquim Plantas, BR-01061970 São Paulo, Brazil
dc.description.affiliationUniv Fed Alfenas, Departamento Ciencias Exatas, LFQM, BR-37130000 Alfenas, MG, Brazil
dc.description.affiliationUnespUNESP Univ Estadual Paulista, Dept Quim, Nucleo Bioensaios Biossintese & Ecofisiol Prod Na, Inst Quim, BR-14801970 Araraquara, SP, Brazil
dc.description.sponsorshipFundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)
dc.description.sponsorshipCoordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)
dc.description.sponsorshipConselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)
dc.description.sponsorshipIdFAPESP: 03/02176-7
dc.format.extent3423-3430
dc.identifierhttp://dx.doi.org/10.2174/092986711796504718
dc.identifier.citationCurrent Medicinal Chemistry. Sharjah: Bentham Science Publ Ltd, v. 18, n. 22, p. 3423-3430, 2011.
dc.identifier.doi10.2174/092986711796504718
dc.identifier.issn0929-8673
dc.identifier.lattes4702004904231248
dc.identifier.orcid0000-0002-1516-7765
dc.identifier.urihttp://hdl.handle.net/11449/26069
dc.identifier.wosWOS:000294405600018
dc.language.isoeng
dc.publisherBentham Science Publ Ltd
dc.relation.ispartofCurrent Medicinal Chemistry
dc.relation.ispartofjcr3.469
dc.relation.ispartofsjr1,015
dc.rights.accessRightsAcesso restrito
dc.sourceWeb of Science
dc.subjectAcetylcholinesterase inhibitionen
dc.subjectanthelmintic activityen
dc.subjectnematicidic activityen
dc.subjectpyridine derivativesen
dc.subjectmolecular hybridizationen
dc.subjectisosterismen
dc.subjectNippostrongylus brasiliensisen
dc.subjectMeloidogyne incognitaen
dc.subjectnatural productsen
dc.titleAnticholinesterasic, Nematostatic and Anthelmintic Activities of Pyridinic and Pyrazinic Compoundsen
dc.typeResenha
dcterms.licensehttp://www.benthamscience.com/permission.php
dcterms.rightsHolderBentham Science Publ Ltd
unesp.author.lattes4702004904231248[11]
unesp.author.orcid0000-0002-1516-7765[11]
unesp.campusUniversidade Estadual Paulista (Unesp), Faculdade de Odontologia, Araraquarapt

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