Examinando por Autor "Quiroga, Jairo"
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Ítem Acceso Abierto Catalyst-, solvent- and desiccant-free three-component synthesis of novel C-2,N-3 disubstituted thiazolidin-4-ones(Elsevier, 2016-12-22) Abonia, Rodrigo; Castillo, Juan; Insuasty, Braulio; Quiroga, Jairo; Sortino, Maximiliano Andrés ; Nogueras, Manuel; Cobo, JustoHerein it is provided an efficient, environmentally friendly and one-pot procedure for the synthesis of a library of new and diversely substituted 1,3 thiazolidin-4-ones in short reaction times and good yields through a solvent-, catalyst- and desiccant-free three-component process. Reactions proceeded by treatment of primary benzyl(aryl)amines with aromatic aldehydes (and ketones) and 2-mercaptoacetic acid acting as both reagent and self-catalyst. All reactions were performed in sand bath instead of the commonly used oil bath avoiding the generation of undesired volatile materials proceeding of the thermal decomposition of the oils. IR, Mass and NMR experiments as well as Xray diffraction confirmed structures of the obtained products.Ítem Acceso Abierto Design of two alternative routes for the synthesis of naftifine and analogues as potential antifungal agents(MDPI, 2018-02-26) Abonia, Rodrigo; Garay, Alexander; Castillo, Juan; Insuasty, Braulio; Quiroga, Jairo; Nogueras, Manuel; Cobo, Justo; Butassi, Estefanía; Zacchino, SusanaÍtem 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 Gabriel; Sortino, Maximiliano Andrés ; Ornelas, Alfredo; Zacchino, Susana; Insuasty, BraulioÍtem 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 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 Synthesis and DFT calculations of novel vanillin-chalcones and their 3-aryl-5-(4-(2- (dimethylamino)- ethoxy)-3-methoxyphenyl)- 4,5-dihydro-1H-pyrazole-1-carbaldehyde derivatives as antifungal agents(MDPI, 2017-09-05) Illicachi, Luis Alberto; Montalvo-Acosta, Joel José; Insuasty, Alberto; Quiroga, Jairo; Abonia, Rodrigo; Sortino, Maximiliano Andrés ; Zacchino, Susana; Insuasty, BraulioÍtem Acceso Abierto Synthesis of Novel Triazine-Based Chalcones and 8,9-dihydro-7H-pyrimido[4,5-b][1,4]diazepines as Potential Leads in the Search of Anticancer, Antibacterial and Antifungal Agents(MDPI, 2024-03-23) Moreno, Leydi M.; Quiroga, Jairo; Abonia, Rodrigo; Crespo Ortíz, María del Pilar; Aranaga, Carlos Andrés; Martínez-Martínez, Luis; Sortino, Maximiliano Andrés; Barreto, Mauricio; Burbano, María E.; Insuasty, Braulio; https://orcid.org/0000-0002-9451-3063; https://orcid.org/0000-0003-3256-0961; https://orcid.org/0000-0003-2160-5167; https://orcid.org/0000-0003-1806-657X; https://orcid.org/0000-0002-6091-4045; https://orcid.org/0000-0002-4271-1690; https://orcid.org/0000-0001-5361-4901; https://orcid.org/0000-0001-8371-3310This study presents the synthesis of four series of novel hybrid chalcones (20,21)a–g and (23,24)a–g and six series of 1,3,5-triazine-based pyrimido[4,5-b][1,4]diazepines (28–33)a–g and the evaluation of their anticancer, antibacterial, antifungal, and cytotoxic properties. Chalcones 20b,d, 21a,b,d, 23a,d–g, 24a–g and the pyrimido[4,5-b][1,4]diazepines 29e,g, 30g, 31a,b,e–g, 33a,b,e–g exhibited outstanding anticancer activity against a panel of 60 cancer cell lines with GI50 values between 0.01 and 100 μM and LC50 values in the range of 4.09 μM to >100 μM, several of such derivatives showing higher activity than the standard drug 5-fluorouracil (5-FU). On the other hand, among the synthesized compounds, the best antibacterial properties against N. gonorrhoeae, S. aureus (ATCC 43300), and M. tuberculosis were exhibited by the pyrimido[4,5-b][1,4]diazepines (MICs: 0.25–62.5 µg/mL). The antifungal activity studies showed that triazinylamino-chalcone 29e and triazinyloxy-chalcone 31g were the most active compounds against T. rubrum and T. mentagrophytes and A. fumigatus, respectively (MICs = 62.5 μg/mL). Hemolytic activity studies and in silico toxicity analysis demonstrated that most of the compounds are safe.