Research Article
Open Access
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
Department of pharmaceutical chemistry, Pune University, Pune, India
M.E.T’s Institute of Pharmacy, Nashik- 422003, Maharashtra, India.
Ashwini H. Pagare et al /Int.J. Chemical Concepts. 2019,5(1),pp 16-24.
Abstract
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.
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