(FBIOyF) Departamento de Química Orgánica
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Ítem Acceso Abierto Synthesis, Bioevaluation and Structural Study of Substituted Phthalazin-1(2H)-ones Acting as Antifungal Agents(MDPI Open Access Publishing, 2013-03) Derita, Marcos; del Olmo, Esther; Barboza, Bianca; García-Cadenas, Ana E.; López-Pérez, José L.; Andújar, Sebastián; Enriz, Daniel; Zacchino, Susana; San Feliciano, ArturoTwenty-five polysubstituted phthalazinone derivatives were synthesized and tested for their antifungal activity against a panel of pathogenic and clinically important yeasts and filamentous fungi. Among them, the compound 4-(4-chlorobenzyl)-2- methylphthalazin-1(2H)-one (5) exhibited a remarkable antifungal activity against standardised strains of dermatophytes and Cryptococcus neoformans, as well as against some clinical isolates. A physicochemical study performed on compound 5 revealed its conformational and electronic characteristics, providing us with useful data for the future design of novel related antifungal analogues.Ítem Acceso Abierto An introductory classroom exercise on protein molecular model visualization and detailed analysis of protein–ligand binding(Wiley, 2013-03-23) Poeylaut-Palena, Andrés A.; Laborde, María de los ÁngelesA learning module for molecular level analysis of protein structure and ligand/drug interaction through the visualization of X-ray diffraction is presented. Using DeepView as molecular model visualization software, students learn about the general concepts of protein structure. This Biochemistry classroom exercise is designed to be carried out by following the detailed instructions that make software handling straightforward. Students learn about protein structure and gain insight into the molecular level of the interaction of two active compounds with their receptor.Ítem Acceso Abierto Effects of Chirality on the Antifungal Potency of Methylated Succinimides Obtained by Aspergillus fumigatus Biotransformations. Comparison with Racemic Ones(MDPI Open Access Publishing, 2013-05-15) Sortino, Maximiliano Andrés ; Postigo, Agustina; Zacchino, SusanaEighteen (3R) and (3R,4R)-N-phenyl-, N-phenylalkyl and N-arylsuccinimides were prepared with high enantioselectivity by biotransformation of maleimides with A. fumigatus. This environmentally friendly, clean and economical procedure was performed by the whole-cell fungal bioconversion methodology. Their corresponding eighteen racemic succinimides were prepared instead by synthetic methods. Both, the racemic and the chiral succinimides were tested simultaneously by the microbroth dilution method of CLSI against a panel of human opportunistic pathogenic fungi of clinical importance. Chiral succinimides showed higher antifungal activity than the corresponding racemic ones and the differences in activity were established by statistical methods. The bottlenecks for developing chiral drugs are how to obtain them through a low-cost procedure and with high enantiomeric excess. Results presented here accomplish both these objectives, opening an avenue for the development of asymmetric succinimides as new antifungal drugs for pharmaceutical use.Ítem Acceso Abierto The type III protein secretion system contributes to Xanthomonas citri subsp. citri biofilm formation(Springer Nature, 2014-04-18) Zimaro, Tamara; Sgro, Germán Gustavo; Garofalo, Cecilia Graciela; Ficarra, Florencia A.; Ottado, Jorgelina; Gottig, Natalia; Thomas, Ludivine; Marondedze, Claudius; Gehring, ChrisBackground: Several bacterial plant pathogens colonize their hosts through the secretion of effector proteins by a Type III protein secretion system (T3SS). The role of T3SS in bacterial pathogenesis is well established but whether this system is involved in multicellular processes, such as bacterial biofilm formation has not been elucidated. Here, the phytopathogen Xanthomonas citri subsp. citri (X. citri) was used as a model to gain further insights about the role of the T3SS in biofilm formation. Results: The capacity of biofilm formation of different X. citri T3SS mutants was compared to the wild type strain and it was observed that this secretion system was necessary for this process. Moreover, the T3SS mutants adhered proficiently to leaf surfaces but were impaired in leaf-associated growth. A proteomic study of biofilm cells showed that the lack of the T3SS causes changes in the expression of proteins involved in metabolic processes, energy generation, exopolysaccharide (EPS) production and bacterial motility as well as outer membrane proteins. Furthermore, EPS production and bacterial motility were also altered in the T3SS mutants. Conclusions: Our results indicate a novel role for T3SS in X. citri in the modulation of biofilm formation. Since this process increases X. citri virulence, this study reveals new functions of T3SS in pathogenesis.Ítem Acceso Abierto New chiral 1,2-aminoalcohols derived from biomass and their application in diethyl zinc additions(Elsevier, 2014-10-15) Zanardi, María Marta; Botta, María Celeste; Suárez, Alejandra GracielaÍtem Acceso Abierto Solvent-free microwave-assisted synthesis of novel pyrazolo[40 ,30 :5,6]pyrido[2,3-d]pyrimidines with potential antifungal activity(Elsevier, 2015-03-17) Acosta, Paola; Insuasty, Braulio; Ortiz, Alejandro; Abonia, Rodrigo; Sortino, Maximiliano Andrés ; Zacchino, Susana; Quiroga, JairoÍtem Acceso Abierto Microwave-assisted synthesis of novel pyrazolo[3,4-g][1,8]naphthyridin-5-amine with potential antifungal and antitumor activity(MDPI, 2015-05-12) Acosta, Paola; Butassi, Estefanía; Insuasty, Braulio; Ortiz, Alejandro; Abonia, Rodrigo; Zacchino, Susana; Quiroga, JairoÍtem Acceso Abierto Synthesis, antiproliferative and antifungal activities of 1,2,3-triazole-substituted carnosic acid and carnosol derivatives(MDPI, 2015-05-14) Pertino, Mariano Walter; Theoduloz, Cristina; Butassi, Estefanía; Zacchino, Susana; Schmeda-Hirschmann, GuillermoÍtem Acceso Abierto Synthesis of new chiral 1,3-aminoalcohols derived from levoglucosenone and their application in asymmetric alkylations(Elsevier, 2015-06-10) Zanardi, María Marta; Suárez, Alejandra GracielaÍtem Acceso Abierto Antifungal activity of pyranonaphthoquinones obtained from Cipura paludosa bulbs(SAGE, 2015-09-01) Campos, Adriana; Rodrigues Souza, Greice Maria; Delle Monache, Franco; Butassi, Estefanía; Zacchino, Susana; Cechinel Filho, ValdirÍtem Acceso Abierto Astringency reduction in red wine by whey proteins(Elsevier, 2015-12-11) Jauregi, Paula; Olatujoye, Jumoke B.; Cabezudo, Ignacio; Frazier, Richard A.; Gordon, Michael H.Ítem Acceso Abierto Antioxidant dietary fibre recovery from Brazilian Pinot noir grape pomace(Elsevier, 2016-01-11) Beres, Carolina; Simas-Tosin, Fernanda F.; Cabezudo, Ignacio; Freitas, Suely P.; Iacomini, Marcello; Mellinger-Silva, Caroline; Cabral, Lourdes M. C.Ítem Acceso Abierto A convenient approach to an advanced intermediate toward the naturally occurring, bioactive 6-substituted 5-hydroxy-4-aryl-1H-quinolin-2-ones(Royal Society of Chemistry, 2016-01-26) Simonetti, Sebastián Osvaldo; Larghi, Enrique Leandro; Kaufman, Teodoro SaúlÍtem Acceso Abierto Development of polymer-supported chiral aminoalcohols derived from biomass and their application to asymmetric alkylation(Elsevier, 2016-04) Botta, María Celeste; Biava, Hernán D.; Spanevello, Rolando Ángel; Mata, Ernesto Gabino; Suárez, Alejandra GracielaÍtem Acceso Abierto Identification of novel chemical scaffolds Inhibiting trypanothione synthetase from pathogenic trypanosomatids(Public Library of Science (PLOS), 2016-04-12) Benítez, Diego; Medeiros, Andrea; Fiestas, Lucía; Panozzo Zénere, Esteban Andrés; Maiwald, Franziska; Prousis, Kyriakos C.; Roussaki, Marina; Calogeropoulou, Theodora; Detsi, Anastasia; Jaeger, Timo; Šarlauskas, Jonas; Peterlin Mašič, Lucíja; Kunick, Conrad; Labadie, Guillermo Roberto; Flohé, Leopold; Comini, Marcelo A.Ítem Acceso Abierto Mebendazole crystal forms in tablet formulations : An ATR-FTIR/chemometrics approach to polymorph assignment(Elsevier, 2016-04-15) Calvo, Natalia Lorena; Kaufman, Teodoro Saúl; Maggio, Rubén MarianoÍtem Acceso Abierto Expedient approach to 6-bromo-2-isopropylidenecoumaranone, a potential intermediate for the synthesis of TMC-120B, pseudodeflectusin, and Their congeners(Wiley, 2016-05-17) Pergomet, Jorgelina Leonor; Kaufman, Teodoro Saúl; Bracca, Andrea Beatriz JuanaÍtem Acceso Abierto Determination of the main solid-state form of albendazole in bulk drug, employing Raman spectroscopy coupled to multivariate analysis(Elsevier, 2016-07-10) Calvo, Natalia Lorena; Arias, Juan Marcelo; Ben Altabef, Aída; Maggio, Rubén Mariano; Kaufman, Teodoro SaúlÍtem Acceso Abierto Hybrid molecules containing a 7-chloro-4-aminoquinoline nucleus and a substituted 2-Pyrazoline with antiproliferative and antifungal activity(MDPI, 2016-07-27) Montoya, Alba; Quiroga, Jairo; Abonia, Rodrigo; Derita, Marcos; Sortino, Maximiliano Andrés ; Ornelas, Alfredo; Zacchino, Susana; Insuasty, BraulioÍtem Acceso Abierto Experimental and theoretical insights in the alkene–arene intramolecular π-stacking interaction(Beilstein-Institut, 2016-07-28) Corne, Valeria; Sarotti, Ariel Marcelo; Ramirez de Arellano, Carmen; Spanevello, Rolando Ángel; Suárez, Alejandra Graciela