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Synthesis and Biological Evaluation of Benzimidazolyl Biphenyl Derivatives as Antihypertensive Agents
Rani S. Kankate, Ashwini H. Pagare, Rohini D. Kakad, Parag S. Gide, Vikas C. Nathe
Recent studies have shown that the interaction between benzimidazole scaffold and angiotensin II receptor may have potential therapeutic benefits. A series of analogues synthesis has been carried out for selected benzimidazole derivatives having electron donor and acceptor substituents 5-nitro, 6-methyl, 6-chloro, 6, 7-dichlorogroup and at 2-position trifluoromethyl, hydroxy ethyl groups and were evaluated for the antihypertensive activity in rats. The authenticity and purity of synthesized have been established through appropriate spectral and chromatographic techniques like TLC, IR, NMR and Mass spectrophotometric methods. Out of all the evaluated compounds, compound 4'-((6-methyl-2-(trifluoromethyl)-1H-benzo[d]imidazol-1-yl) methyl)-[1, 1’-biphenyl]-2-carboxylic acid (3b) showed improved antihypertensive activity. Biological activity of synthesized compounds was carried out using rat blood pressure measurement experiment i.e. noninvasive blood pressure(NIBP); induction of hypertension developed by administration of corticosteroid dexamethasone intramuscularly. The maximum fall in blood pressure produced by standard drug losartan was compare with synthesized compounds. Finally it is concluded that different substituted benzimidazole derivatives has appreciable and selective action against angiotensin II induced hypertension. Keywords : Benzimidazole, Biphenyl,Tetrazole, Antihypertensive activity, angiotensin II.[Full Text Article]