Synthesis and smooth muscle calcium channel antagonist effects of new derivatives of 1, 4 - dihydropyridine containing nitroimidazolyl substituent
DARU-Journal of Faculty of Pharmacy Tehran University of Medical Sciences. 2002; 10 (3): 130-6
en Inglés
| IMEMR
| ID: emr-59121
ABSTRACT
A group of racemic 3-[[2-hydroxyethyl], [2-Methoxyethyl], [2-acetylethyl] or [2-cyanoethyl]], 5- methyl, ethyl or isopropyl-1, 4-dihydro-2, 6-dimethyl-4-[1-methyl-5-nitro-2-imidazolyl]-3, 5-pyridinedicarboxylates [XIV-XXV] were prepared by the reaction of 1-methyl-5-nitroimidazol-2-carboxaldehyde [X] with acetoacetic esters [VI-IX] and alkys 3-aminocrotonate [XI-XIII]. In vitro calcium channel antagonist activities of the tested compounds were determined by their effects on contraction of Guinea Pig Ileal Longitudinal Smooth Muscle [GPILSM] which was induced by carbacol [1.67 = 10 -7 M]. All compounds exhibited calcium channel antagonist activity [IC50=10 -12 to 10 -13 M range] comparable to nifedipine as reference drug [IC50=1.07 +/- 0.12x 10 -11 M]
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Índice:
IMEMR (Mediterraneo Oriental)
Asunto principal:
Bloqueadores de los Canales de Calcio
/
Cobayas
/
Íleon
/
Músculo Liso
/
Acetoacetatos
/
Nitroimidazoles
Límite:
Animales
Idioma:
Inglés
Revista:
J. Fac. Pharm. Tehran Univ. Med. Sci.
Año:
2002
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