Design, synthesis, and pharmacological evaluation of 4'-{2-[4-[3- chloro-2-(substituted-phenyl)-4-oxo-azetidin-1-yl)-phenyl]- benzoimidazol-1-ylmethyl}-biphenyl-2-carboxylic acids

Series of non peptide angiotensin (A-II) receptor antagonist has been prepared by 4'-{2-[4-[3- chloro-2-(substituted-phenyl)-4-oxo-azetidin-1-yl)-phenyl]-benzoimidazol-1-yl-methyl}-biphenyl- 2-carboxylic acid were synthesised by 2-(4-aminophenyl) Benzimidazole (0.01 mol), substituted Benzaldehyde (0.01 mol) and a drop of acetic acid was dissolved in ethanol (25 ml) and heated on a steam bath for 45-60 min Chloroacetyl chloride (0.01mol) was added drop wise to a mixture of schiff base (0.01mol) and triethylamine (0.02 mol) in dioxane (25 ml) at room temperature Schiff bases react with biphenyl carboxylic acid with different substituents aryl group cyclocondensation with appropriate reagents. Different from the previously reported and related compounds in that they produce a potent hypertensive effect The compounds synthesised were identified by 1H NMR, 13C NMR, FAB Mass and FT-IR spectroscopic techniques. All compounds studied in this work were screened for their antihypertensive activity by tail cuff method and direct method measurement of Blood pressure.

Author(s): M. C. Sharma, D. V. Kohlia, Smita Sharmab and A. D. Sharma

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