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Synthesis, In Vitro, In Vivo and In Silico Antidiabetic Bioassays of 4-Nitro(thio)phenoxyisobutyric Acids Acting as Unexpected PPAR? Modulators: An In Combo Study

dc.contributor.authorColín Lozano, Blanca
dc.contributor.authorTorres Gómez, Héctor
dc.contributor.authorHidalgo Figueroa, Sergio Nemorio
dc.contributor.authorChávez Silva, Fabiola
dc.contributor.authorEstrada Soto, Samuel
dc.contributor.authorAlmanza Pérez, Julio Cesar
dc.contributor.authorNavarrete Vázquez, Gabriel
dc.date.accessioned2023-06-14T16:12:29Z
dc.date.available2023-06-14T16:12:29Z
dc.date.issued2022
dc.identifier.citationColin-Lozano, B.; Torres-Gomez, H.; Hidalgo-Figueroa, S.; Chávez-Silva, F.; Estrada-Soto, S.; Almanza-Pérez, J.C.; Navarrete-Vazquez, G. Synthesis, In Vitro, In Vivo and In Silico Antidiabetic Bioassays of 4-Nitro(thio)phenoxyisobutyric Acids Acting as Unexpected PPAR? Modulators: An In Combo Study. Pharmaceuticals 2022, 15, 102. https://doi.org/10.3390/ph15010102
dc.identifier.urihttp://hdl.handle.net/11627/6351
dc.description.abstract"Four isobutyric acids (two nitro and two acetamido derivatives) were prepared in two steps and characterized using spectral analysis. The mRNA concentrations of PPAR? and GLUT-4 (two proteins documented as key diabetes targets) were increased by 3T3-L1 adipocytes treated with compounds 1–4, but an absence of in vitro expression of PPAR? was observed. Docking and molecular dynamics studies revealed the plausible interaction between the synthesized compounds and PPAR?. In vivo studies established that compounds 1–4 have antihyperglycemic modes of action associated with insulin sensitization. Nitrocompound 2 was the most promising of the series, being orally active, and one of multiple modes of action could be selective PPAR? modulation due to its extra anchoring with Gln-286. In conclusion, we demonstrated that nitrocompound 2 showed strong in vitro and in vivo effects and can be considered as an experimental antidiabetic candidate."
dc.publisherMDPI
dc.rightsAttribution-NonCommercial-NoDerivatives 4.0 Internacional
dc.rights.urihttp://creativecommons.org/licenses/by-nc-nd/4.0/
dc.subjectPPAR
dc.subjectDrug design
dc.subjectDiabetes
dc.subjectMolecular dynamics
dc.subject.classificationFARMACOLOGÍA
dc.titleSynthesis, In Vitro, In Vivo and In Silico Antidiabetic Bioassays of 4-Nitro(thio)phenoxyisobutyric Acids Acting as Unexpected PPAR? Modulators: An In Combo Study
dc.typearticle
dc.identifier.doihttps://doi.org/10.3390/ph15010102
dc.rights.accessAcceso Abierto


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Attribution-NonCommercial-NoDerivatives 4.0 Internacional
Except where otherwise noted, this item's license is described as Attribution-NonCommercial-NoDerivatives 4.0 Internacional