Solvent-free microwave-assisted synthesis of novel pyrazolo[40 ,30 :5,6]pyrido[2,3-d]pyrimidines with potential antifungal activity

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dc.creator Acosta, Paola
dc.creator Insuasty, Braulio
dc.creator Ortiz, Alejandro
dc.creator Abonia, Rodrigo
dc.creator Sortino, Maximiliano
dc.creator Zacchino, Susana
dc.creator Quiroga, Jairo
dc.date.accessioned 2020-12-17T00:24:15Z
dc.date.available 2020-12-17T00:24:15Z
dc.date.issued 2015-03-17
dc.identifier.issn 1878-5352 es
dc.identifier.uri http://hdl.handle.net/2133/19493
dc.description Novel fused pyrazolo[40 ,30 :5,6]pyrido[2,3-d]pyrimidines 5 were prepared by a solvent-free microwave assisted reaction of heterocyclic o-aminonitriles 3 and cyanopyridines 4 in the presence of tBuOK as catalyst. This protocol provides a versatile procedure for the synthesis of the title compounds with the advantages of easy work-up, mild reaction conditions and good yields. All compounds were also tested for antifungal properties against two clinically important fungi; Candida albicans and Cryptococcus neoformans. Several compounds showed moderate activity against both fungi, being 5a the most active compound. Analysis of the antifungal behavior of properly grouped compounds allowed to determine that the position of the N in the pyrimidyl moiety per se does not play a role in the activity. In turn, the type of 4-R substituent appears to influence the activity. In addition to the above considerations, the lipophilicity of compounds measured as logP showed to be not related to the activity and regarding the dipole moment (D), no net correlation was observed, although it is the most active compounds (% inhibition >50%) that have a D P 7.5, mainly against C. albicans. es
dc.description.sponsorship Departamento Administrativo de Ciencia, Tecnología e Innovación (Colciencias) es
dc.description.sponsorship Universidad del Valle es
dc.format application/pdf
dc.format.extent 481-492 es
dc.language.iso eng es
dc.publisher Elsevier es
dc.rights openAccess es
dc.rights.uri https://creativecommons.org/licenses/by-nc-nd/4.0/ *
dc.subject Pyrazolo-Pyrido-Pyrimidine es
dc.subject o-Aminonitriles es
dc.subject Cyanopyridines es
dc.subject Microwave Irradiation es
dc.subject Antifungal Activity es
dc.title Solvent-free microwave-assisted synthesis of novel pyrazolo[40 ,30 :5,6]pyrido[2,3-d]pyrimidines with potential antifungal activity es
dc.type article
dc.type artículo
dc.type publishedVersion
dc.rights.holder Universidad Nacional de Rosario es
dc.rights.holder Acosta, Paola es
dc.rights.holder Insuasty, Braulio es
dc.rights.holder Ortiz, Alejandro es
dc.rights.holder Abonia, Rodrigo es
dc.rights.holder Sortino, Maximiliano es
dc.rights.holder Zacchino, Susana es
dc.rights.holder Quiroga, Jairo es
dc.relation.publisherversion https://doi.org/10.1016/j.arabjc.2015.03.002 es
dc.relation.publisherversion https://www.sciencedirect.com/science/article/pii/S1878535215000714?via%3Dihub es
dc.rights.text Attribution-NonCommercial-NoDerivatives 4.0 International (CC BY-NC-ND 4.0) es
dc.citation.title Arabian Journal of Chemistry es
dc.citation.volume 9(3) es
dc.description.fil Fil: Acosta, Paola. Universidad del Valle. Facultad de Ciencias Naturales y Exactas. Departamento de Química. Grupo de Investigación de Compuestos Heterocíclicos (GICH); Colombia. es
dc.description.fil Fil: Insuasty, Braulio. Universidad del Valle. Facultad de Ciencias Naturales y Exactas. Departamento de Química. Grupo de Investigación de Compuestos Heterocíclicos (GICH); Colombia. es
dc.description.fil Fil: Ortiz, Alejandro. Universidad del Valle. Facultad de Ciencias Naturales y Exactas. Departamento de Química. Grupo de Investigación de Compuestos Heterocíclicos (GICH); Colombia. es
dc.description.fil Fil: Abonia, Rodrigo. Universidad del Valle. Facultad de Ciencias Naturales y Exactas. Departamento de Química. Grupo de Investigación de Compuestos Heterocíclicos (GICH); Colombia. es
dc.description.fil Fil: Sortino, Maximiliano. Universidad Nacional de Rosario. Facultad de Farmacia y Bioquímica. Área Farmacognosia; Argentina. es
dc.description.fil Fil: Zacchino, Susana. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Área Farmacognosia; Argentina. es
dc.description.fil Fil: Quiroga, Jairo. Universidad del Valle. Facultad de Ciencias Naturales y Exactas. Departamento de Química. Grupo de Investigación de Compuestos Heterocíclicos (GICH); Colombia. es
dc.type.collection articulo
dc.type.version publishedVersion es


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