SYNTHESIS AND BIOLOGICAL EVALUATION OF BENZIMIDAZOLYL BIPHENYL DERIVATIVES AS AN ANTIHYPERTENSIVE AGENT Authors: Kapse SN , PAGARE AH, MALPURE PS*, VYAVHARE PV AND TALELE GS
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 Publication date: 01/01/2023 https://ijbpas.com/pdf/2023/January/MS_IJBPAS_2023_6592.pdfDownload PDFhttps://doi.org/10.31032/IJBPAS/2023/12.1.6592