Persona:
López Peláez, Antonio

Cargando...
Foto de perfil
Dirección de correo electrónico
ORCID
0000-0003-0908-4821
Fecha de nacimiento
Proyectos de investigación
Unidades organizativas
Puesto de trabajo
Apellidos
López Peláez
Nombre de pila
Antonio
Nombre

Resultados de la búsqueda

Mostrando 1 - 2 de 2
  • Publicación
    Synthesis, structure and biological activity of 3(5)-trifluoromethyl-1H-pyrazoles derived from hemicurcuminoids
    (Elsevier, 2015-11-14) Cabildo Miranda, Mª del Pilar; Cornago, María del Pilar; Sanz, D.; Claramunt, R. M.; Alkorta, Ibon; Elguero, J.; Garcia, J. A.; Acuña Castroviejo, Darío; Nieto Gómez, Carla Isabel::virtual::3403::600; López Peláez, Antonio::virtual::3404::600; Nieto Gómez, Carla Isabel; López Peláez, Antonio; Nieto Gómez, Carla Isabel; López Peláez, Antonio; Nieto Gómez, Carla Isabel; López Peláez, Antonio
    Six new 3(5)-trifluoromethyl-5(3)-substituted-styryl-1H-pyrazoles have been synthesized and their tautomerism studied in solution and in the solid state. The determination of their structures has been based on multinuclear NMR spectroscopy together with GIAO/B3LYP/6–311++G(d,p) theoretical calculations of eight structures for each pyrazole (two tautomers and four conformations). Five out of the six compounds present inhibition percentages of the iNOS isoform higher than 50%. With regard to the nNOS inhibitory activity, only two of the studied compounds show an inhibition of about 50%. Finally, concerning the eNOS, there is a compound presenting a low percentage of inhibition (40.2%) attaining in the other cases 50%.
  • Publicación
    Fluorination Effects on NOS Inhibitory Activity of Pyrazoles Related to Curcumin
    (MDPI, 2015-08-28) Cabildo Miranda, Mª del Pilar; Cornago, María del Pilar; Sanz, D.; Claramunt, R. M.; Torralba, M. Carmen; Torres, M. Rosario; Elguero, J.; Garcia, J. A.; Acuña Castroviejo, Darío; Nieto Gómez, Carla Isabel; López Peláez, Antonio
    A series of new (E)-3(5)-[β-(aryl)-ethenyl]-5(3)-phenyl-1H-pyrazoles bearing fluorine atoms at different positions of the aryl group have been synthesized starting from the corresponding β-diketones. All compounds have been characterized by elemental analysis, DSC as well as NMR (1H, 13C, 19F and 15N) spectroscopy in solution and in solid state. Three structures have been solved by X-ray diffraction analysis, confirming the tautomeric forms detected by solid state NMR. The in vitro study of their inhibitory potency and selectivity on the activity of nNOS and eNOS (calcium-calmodulin dependent) as well as iNOS (calcium-calmodulin independent) isoenzymes is presented. A qualitative structure–activity analysis allowed the establishment of a correlation between the presence/absence of different substituents with the inhibition data proving that fluorine groups enhance the biological activity. (E)-3(5)-[β-(3-Fluoro-4-hydroxyphenyl)-ethenyl]-5(3)-phenyl-1H-pyrazole (13), is the best inhibitor of iNOS, being also more selective towards the other two isoforms.