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000Synthesis of new α-aminophosphonates: Evaluation as anti-inflammatory agents and QSAR studies

Romero-Estudillo, Ivan ; Viveros-Ceballos, José Luis ; Cazares-Carreño, Obed ; González-Morales, Angelina ; de Jesús, Berenice Flores ; López-Castillo, Misael ; Razo-Hernández, Rodrigo Said ; Castañeda-Corral, Gabriela ; Ordóñez, Mario

Bioorganic & medicinal chemistry, 2019-06, Vol.27 (12), p.2376-2386 [Periódico revisado por pares]

England: Elsevier Ltd

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  • Título:
    000Synthesis of new α-aminophosphonates: Evaluation as anti-inflammatory agents and QSAR studies
  • Autor: Romero-Estudillo, Ivan ; Viveros-Ceballos, José Luis ; Cazares-Carreño, Obed ; González-Morales, Angelina ; de Jesús, Berenice Flores ; López-Castillo, Misael ; Razo-Hernández, Rodrigo Said ; Castañeda-Corral, Gabriela ; Ordóñez, Mario
  • Assuntos: Anti-inflammatory effect ; Dose-response relationship ; QSAR ; Three component reaction ; α-Aminophosphonates
  • É parte de: Bioorganic & medicinal chemistry, 2019-06, Vol.27 (12), p.2376-2386
  • Notas: ObjectType-Article-2
    SourceType-Scholarly Journals-1
    ObjectType-Undefined-1
    ObjectType-Feature-3
    content type line 23
  • Descrição: [Display omitted] In this paper, we report the synthesis of a new series of α-aminophosphonates derivatives based in an efficient three-component reaction. All compounds prepared showed significant anti-inflammatory activity, being the compounds 1a, 1c, 1d, 1f, 2b and 2c the most promising ones, in terms of maximal efficacy (over 95%), potency (ED50 range between 0.7 and 10.1 mg/ear) and relative potency (range from 0.04 to 0.67). Compounds 1a, 1c, 1d and 1f significantly decrease the number of neutrophils (range from 46.7 to 63.0%) and monocytes (18.9–34.1%) in blood samples from the orbital sinus. Additionally, QSAR model revealed that the spherical molecular shape and the location of the HOMO on the phenyl ring improves the anti-inflammatory activity of the compounds. The values of R2, Q2, s and F statistical parameters and the QUIK, asymptotic Q2 and Overfitting rules validate the descriptive and predictive ability of the QSAR model. Altogether these results suggest that these new α-aminophosphonates are potential agents for the treatment of inflammation.
  • Editor: England: Elsevier Ltd
  • Idioma: Inglês
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