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12 results on '"Tapia, Alejandro"'

2. A New Series of Antibacterial Nitrosopyrimidines: Synthesis and 3 Structure?Activity Relationship

Author

Olivella, Monica, Marchal, Antonio, Nogueras, Manuel, Melguizo, Manuel, Lima, Beatriz Viviana, Tapia, Alejandro, Feresin, Gabriela Egly, Parravicini, Oscar, Giannini, Fernando, Andujar, Sebastian Antonio, Cobo, Justo, and Enriz, Ricardo Daniel

Subjects
Química Orgánica, Ciencias Químicas, Conformational and electronic analysis, 4,6-Bis(alkyl or arylamino)-5-nitrosopyrimidines, CIENCIAS NATURALES Y EXACTAS, Antibacterial compounds, SAR
Abstract

New nitrosopyrimidines were synthesized and evaluated as potential antibacterial agents. Different compounds structurally related with 4,6-bis(alkyl or arylamino)-5-nitrosopyrimidines were evaluated. Some of these nitrosopyrimidines displayed significant antibacterial activity against human pathogenic bacteria. Among them compounds 1c, 2a–c, and 9a–c exhibited remarkable activity against methicillin-sensitive and -resistant Staphylococcus aureus, Escherichia coli, Yersinia enterocolitica, and Salmonella enteritidis. A detailed structure–activity relationship study, supported by theoretical calculations, aided us to identify and understand the minimal structural requirements for the antibacterial action of the nitrosopyrimidines reported here. Thus, our results have led us to identify a topographical template that provides a guide for the design of new nitrosopyrimidines with antibacterial effects. Fil: Olivella, Monica. Universidad Nacional de San Luis. Facultad de Química, Bioquímica y Farmacia; Argentina Fil: Marchal, Antonio. Universidad de Jaén; España Fil: Nogueras, Manuel. Universidad de Jaén; España Fil: Melguizo, Manuel. Universidad de Jaén; España Fil: Lima, Beatriz Viviana. Universidad Nacional de San Juan. Facultad de Ingeniería. Instituto de Biotecnología; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina Fil: Tapia, Alejandro. Universidad Nacional de San Juan. Facultad de Ingeniería. Instituto de Biotecnología; Argentina Fil: Feresin, Gabriela Egly. Universidad Nacional de San Juan. Facultad de Ingeniería. Instituto de Biotecnología; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina Fil: Parravicini, Oscar. Universidad Nacional de Tucumán. Facultad de Bioquímica, Química y Farmacia. Instituto de Química Orgánica; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina Fil: Giannini, Fernando. Universidad Nacional de San Luis. Facultad de Química, Bioquímica y Farmacia; Argentina Fil: Andujar, Sebastian Antonio. Universidad Nacional de San Luis. Facultad de Química, Bioquímica y Farmacia; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico San Luis. Instituto Multidisciplinario de Investigaciones Biológicas de San Luis; Argentina Fil: Cobo, Justo. Universidad de Jaén; España Fil: Enriz, Ricardo Daniel. Universidad Nacional de San Luis. Facultad de Química, Bioquímica y Farmacia; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico San Luis. Instituto Multidisciplinario de Investigaciones Biológicas de San Luis; Argentina

Published
2015
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3. Small Peptides Derived from Penetratin as Antibacterial Agents

Author

Parravicini, Oscar, primary, Somlai, Csaba, additional, Andujar, Sebastián A., additional, Garro, Adriana D., additional, Lima, Beatriz, additional, Tapia, Alejandro, additional, Feresin, Gabriela, additional, Perczel, Andras, additional, Tóth, Gabor, additional, Cascales, Javier López, additional, Rodríguez, Ana M., additional, and Enriz, Ricardo D., additional

Published
2016
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4. A New Series of Antibacterial Nitrosopyrimidines: Synthesis and Structure-Activity Relationship

Author

Olivella, Monica, primary, Marchal, Antonio, additional, Nogueras, Manuel, additional, Melguizo, Manuel, additional, Lima, Beatriz, additional, Tapia, Alejandro, additional, Feresin, Gabriela E., additional, Parravicini, Oscar, additional, Giannini, Fernando, additional, Andujar, Sebastián A., additional, Cobo, Justo, additional, and Enriz, Ricardo D., additional

Published
2014
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6. Penetratin and Derivatives Acting as Antibacterial Agents

Author

Garro, Adriana D., primary, Olivella, Mónica S., additional, Bombasaro, José A., additional, Lima, Beatriz, additional, Tapia, Alejandro, additional, Feresin, Gabriela, additional, Perczel, Andras, additional, Somlai, Csaba, additional, Penke, Botond, additional, López Cascales, Javier, additional, Rodríguez, Ana M., additional, and Enriz, Ricardo D., additional

Published
2013
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7. Essential Oil of Azorella cryptantha Collected in Two Different Locations from San Juan Province, Argentina: Chemical Variability and Anti‐Insect and Antimicrobial Activities

Author

López, Sandra, primary, Lima, Beatriz, additional, Aragón, Liliana, additional, Espinar, Luis Ariza, additional, Tapia, Alejandro, additional, Zacchino, Susana, additional, Zygadlo, Julio, additional, Feresin, Gabriela Egly, additional, and López, María Liza, additional

Published
2012
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8. Essential Oils of Medicinal Plants from the Central Andes of Argentina: Chemical Composition, and Antifungal, Antibacterial, and Insect-Repellent Activities

Author

Lima, Beatriz, primary, López, Sandra, additional, Luna, Lorena, additional, Agüero, María B., additional, Aragón, Liliana, additional, Tapia, Alejandro, additional, Zacchino, Susana, additional, López, María L., additional, Zygadlo, Julio, additional, and Feresin, Gabriela E., additional

Published
2011
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12. A new antifungal and antiprotozoal depside from the Andean lichen Protousnea poeppigii.

Author

Schmeda-Hirschmann G, Tapia A, Lima B, Pertino M, Sortino M, Zacchino S, Arias AR, and Feresin GE

Subjects
Animals, Anti-Infective Agents chemistry, Anti-Infective Agents isolation & purification, Ascomycota chemistry, Depsides chemistry, Drug Evaluation, Preclinical methods, Magnetic Resonance Spectroscopy, Microbial Sensitivity Tests, Salicylates pharmacology, Usnea chemistry, Anti-Infective Agents pharmacology, Bacteria drug effects, Depsides pharmacology, Leishmania drug effects, Lichens chemistry, Mitosporic Fungi drug effects
Abstract

Extracts from the Andean lichens Protousnea poeppigii and Usnea florida displayed antimicrobial activity against the pathogenic fungi Microsporum gypseum, Trichophyton mentagrophytes and T. rubrum with MIC values between 50 and 100 microg/mL. From the active extracts, four main metabolites were isolated and identified as the new depside, isodivaricatic acid, and the known metabolites 5-propylresorcinol, divaricatinic acid and usnic acid. Isodivaricatic acid and divaricatinic acid presented antifungal effect towards M. gypseum with a MIC of 50 microg/mL and against T. mentagrophytes and T. rubrum and with MIC values of 50 and 100 microg/mL, respectively. The new isodivaricatic acid was active towards Leishmania amazonensis, Leishmania brasiliensis and Leishmania infantum promastigotes with 100% lysis at 100 microg/mL.The activity of the new compound decreased on acetylation of the hydroxy groups as well as on methylation of the acid function. The structures were elucidated by spectroscopic means. The spectroscopic data of isodivaricatic acid are presented here for the first time.

Published
2008
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