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

نویسندگان

  • Farzin Hadizadeh Biotechnology 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
  • Mahmoud Seifi Biotechnology 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
  • Seyed Ahmad Mohajeri 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 مقاله:

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-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 ', 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

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

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

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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

دوره 14  شماره 5

صفحات  451- 457

تاریخ انتشار 2011-09-01

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