Your browser doesn't support javascript.
loading
Mostrar: 20 | 50 | 100
Resultados 1 - 2 de 2
Filtrar
Más filtros










Base de datos
Intervalo de año de publicación
1.
Arch Pharm (Weinheim) ; 352(12): e1900187, 2019 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-31583763

RESUMEN

A series of the morpholine-liganded palladium(II) complexes (1a-e) bearing N-heterocyclic carbene (NHC) functionalized by benzonitrile were synthesized. These complexes were synthesized from (NHC)Pd(II)(pyridine) complexes (PEPPSI) and morpholine. The new complexes were fully characterized by using 1 H NMR, 13 C NMR, Fourier-transform infrared spectroscopy, and elemental analysis techniques. Single-crystal X-ray diffraction was used to determine the structure of a derivative. The DNA-binding studies of the new (NHC)Pd(II)morpholine complexes were examined using the pBR322 plasmid. The 2,4,6-trimethylbenzyl derivative compound has the most DNA binding activity. In addition, for the 3-methylbenzyl derivative compound, oxidation effects were observed at concentrations higher than 100 µg/ml. Also, the molecular and crystal structures of the complex 3-methylbenzyl derivative compound were recorded by using a single-crystal X-ray diffraction method.


Asunto(s)
Complejos de Coordinación/síntesis química , Metano/análogos & derivados , Morfolinas/síntesis química , Paladio/química , Sitios de Unión , Complejos de Coordinación/química , Complejos de Coordinación/farmacología , Cristalografía por Rayos X , ADN Circular/química , Ligandos , Metano/química , Morfolinas/química , Morfolinas/farmacología , Nitrilos/química , Plásmidos/química
2.
Arch Pharm (Weinheim) ; 351(7): e1800029, 2018 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-29963738

RESUMEN

meta-Cyanobenzyl-substituted N-heterocyclic carbene (NHC) precursors were synthesized by the reaction of a series of N-(alkyl)benzimidazolium with 3-bromomethyl-benzonitrile. These benzimidazolium salts were characterized by using 1 H NMR, 13 C NMR, FTIR spectroscopy, and elemental analysis techniques. The molecular and crystal structures of 2f and 2g complexes were obtained by using the single-crystal X-ray diffraction method. The derivatives of these novel NHC precursors were effective inhibitors of α-glycosidase (AG), the cytosolic carbonic anhydrase I and II isoforms (hCA I and II), butyrylcholinesterase (BChE), and acetylcholinesterase (AChE) with Ki values in the range of 1.01-2.12 nM for AG, 189.56-402.44 nM for hCA I, 112.50-277.37 nM for hCA II, 95.45-352.58 nM for AChE, and 132.91-571.18 nM for BChE. In the last years, inhibition of the CA enzyme has been considered as a promising factor for pharmacologic intervention in a diversity of disturbances such as obesity, glaucoma, cancer, and epilepsy.


Asunto(s)
Butirilcolinesterasa/efectos de los fármacos , Inhibidores de Anhidrasa Carbónica/farmacología , Inhibidores de la Colinesterasa/farmacología , Inhibidores de Glicósido Hidrolasas/farmacología , Bencimidazoles/síntesis química , Bencimidazoles/química , Bencimidazoles/farmacología , Compuestos de Bencilo/síntesis química , Compuestos de Bencilo/química , Compuestos de Bencilo/farmacología , Butirilcolinesterasa/metabolismo , Inhibidores de Anhidrasa Carbónica/síntesis química , Inhibidores de Anhidrasa Carbónica/química , Inhibidores de la Colinesterasa/síntesis química , Inhibidores de la Colinesterasa/química , Cristalización , Inhibidores de Glicósido Hidrolasas/síntesis química , Inhibidores de Glicósido Hidrolasas/química , Espectroscopía de Resonancia Magnética/métodos , Espectroscopía Infrarroja por Transformada de Fourier/métodos , Relación Estructura-Actividad , Difracción de Rayos X
SELECCIÓN DE REFERENCIAS
DETALLE DE LA BÚSQUEDA
...