synthesis of novel 4-[1-(4-fluorobenzyl)-5-imidazolyl] dihydropyridines and studying their effects on rat blood pressure

نویسندگان

seyed ahmad mohajeri pharmaceutical research center, school of pharmacy, mashhad university of medical sciences, mashhad, iran

hossein hosseinzadeh pharmaceutical research center, school of pharmacy, mashhad university of medical sciences, mashhad, iran

sara salami pharmaceutical research center, school of pharmacy, mashhad university of medical sciences, mashhad, iran

vahidehsadat motamedshariaty pharmaceutical research center, school of pharmacy, mashhad university of medical sciences, mashhad, iran

چکیده

objective(s) calcium-channel blockers have an important role in the treatment of several cardiovascular disorders. derivatives of 1, 4-dihydropyridine are one of the most potent calcium antagonists. in this study four novel &apos;, 4-dihydropyridine calcium channel blockers were synthesized and their hypotensive properties were investigated in male rats. materials and methods four 1, 4-dihydropyridines bearing 1-(4-fluorobenzyl)-5-imidazolyl substituent at 4 position (5a-d) were synthesized and tested for hypotensive activity in male rats. the animal was anaesthetized and the right jugular vein was cannulated for the administration of test agents. the left carotid artery was cannulated and connected to a pressure transducer for continuous monitoring of arterial blood pressure. results all synthesized compounds lowered rat blood pressure significantly in comparison with dmso as vehicle and nifedipine as positive control. the hypotensive effects of all compounds were less than that of nifedipine at 2 and 4 mg/kg (p< 0.05). the order of their effects on mean arterial blood pressure (mabp) was 5b>5c>5a>5d at dose of 4 mg/kg (p< 0.05). all compounds tested increased heart rate in comparison with dmso (p< 0.05). the chronotropic effect of nifedipine was significantly less than synthesized compounds at dose of 4 mg/kg (p< 0.01). conclusion the results showed that these novels &apos;, 4-dihydropyridines decreased mean arterial blood pressure (mabp) significantly, while increased heart rate in rat.

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منابع مشابه

Synthesis of Novel 4-[1-(4-fluorobenzyl)-5-imidazolyl] Dihydropyridines and Studying their Effects on Rat Blood Pressure

Objective(s) Calcium-channel blockers have an important role in the treatment of several cardiovascular disorders. Derivatives of 1, 4-dihydropyridine are one of the most potent calcium antagonists. In this study four novel ', 4-dihydropyridine calcium channel blockers were synthesized and their hypotensive properties were investigated in male rats. Materials and Methods Four 1, 4-dihydropyr...

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Synthesis of Novel 4-[1-(4-fluorobenzyl)-5-imidazolyl] Dihydropyridines and Studying their Effects on Rat Blood Pressure

OBJECTIVES Calcium-channel blockers have an important role in the treatment of several cardiovascular disorders. Derivatives of 1, 4-dihydropyridine are one of the most potent calcium antagonists. In this study four novel 1, 4-dihydropyridine calcium channel blockers were synthesized and their hypotensive properties were investigated in male rats. MATERIALS AND METHODS Four 1, 4-dihydropyridi...

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synthesis and antihypertensive activity of novel 4-[1-(4-x-benzyl)-5-imidazolyl] dihydropyridines in rat

a series of 1,4-dihydropyridine calcium channel blockers bearing 1-(4-x -benzyl)-5-imidazolyl substituent at 4 position (5a-e) (x=h, f) were synthesized and tested for antihypertensive activity in desoxycorticosterone acetate (doca)-induced hypertension in rats. amlodipine was used as the standard dihydropyridine. all compounds tested showed lower antihypertensive activity than that of amlodipi...

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SYNTHESIS OF 4-(1-BENZYL-5-IMIDAZOLYL)-1,4-DIHYDROPYRIDINES

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Effects of 4-(2-Alkylthio-1-benzyl-5-imidazolyl)-Dihydropyridines on the Isolated Rat Colon and Right Atrium Contractility

Objectives In order to provide a pharmacological profile for some newly synthesized dihydropyridines, we investigated their effects on the isolated rat colon segments and the isolated rat atrium contractility. The tested compounds include alkyl ester analogues of nifedipine, in which the ortho-nitrophenyl group at position 4 is replaced by 2-alkylthio-1-benzyl-5-imidazolyl substituent, and nif...

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synthesis of 4-(1-benzyl-5-imidazolyl)-1,4-dihydropyridines

the o-nitrophenyl group at position 4 of dihydropyridine of nifedipine analogues was replaced with 2-alkylthio-1-benzyl-5-imidazolyl substituent. starting from dihydroxyacetone 2-alkythio-1-benzyl- 5-formyl imidazole (3) was first synthesized which was subsequently used in synthesizing symmetrical (5a-f) and asymmetrical (6a,b) dihydropyridines. primarily pharmacological studies of the title co...

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عنوان ژورنال:
iranian journal of basic medical sciences

جلد ۱۴، شماره ۵، صفحات ۴۵۱-۴۵۷

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