@SYNTHESIS AND SMOOTH MUSCLE CALCIUM CHANNEL ANTAGONIST EFFECT OF ALKYL, AMINOALKYL 1,4-DIHYDRO-2,6-DIMETHYL-4-NITROIMIDAZOLE-3,5 PYRIDINE DICARBOXYLATES

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MIRI R.; SHAFIEI A.; NIKNAHAD H.; VAZIN A.; AZARPIRA A.

مرکز اطلاعات علمی Scientific Information Database (SID) - Trusted Source for Research and Academic Resources

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Journal: DARU Journal of Pharmaceutical Sciences Year:2002 | Volume:10 | Issue:3 Page(s): 40-45

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Title

@SYNTHESIS AND SMOOTH MUSCLE CALCIUM CHANNEL ANTAGONIST EFFECT OF ALKYL, AMINOALKYL 1,4-DIHYDRO-2,6-DIMETHYL-4-NITROIMIDAZOLE-3,5 PYRIDINE DICARBOXYLATES

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Keywords

CA+² CHANNEL ANTAGONIST

NITROIMIDAZOLE

DHP

ARYLPIPERAZINE

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 alkyl 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 x 10-7 M). All compounds exhibited calcium channel antagonist activity (IC5o=10-12 to 10-13M range) comparable to nifedipine as reference drug (IC5o=1.07±0.12 x 10 -11 M).

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