| 摘要 |
<p>PURPOSE: Non-peptide compounds having bradykinin antagonistic activity, a preparation method thereof and a pharmaceutical composition containing the same are provided. The compounds are useful for prevention and treatment of diseases caused by bradykinin. CONSTITUTION: Non-peptide compounds having bradykinin antagonistic activity represented by the formula 1 and pharmaceutically acceptable salts thereof are provided, wherein R1 is isopropyl, benzyl, 4-methylbenzyl, 4-methoxybenzyl, 1-methyl-3-phenyl propyl, 3,4,5-trimethoxybenzyl, 2-(4-(4-chlorophenyl)thiazole), 3-(5-t-benzoisoxazole), 2-(4-(4-bromophenyl)thiazole), cyclohexyl, 5-(3-methylisooxazole), 3,4-dibenzyloxyphenethyl; R2 is H, R3CO; and R3 is methyl, phenyl, benzyl, naphthyl(C10H7), or C10H7CH2. A method for preparing the non-peptide compounds comprises the steps of: (1) in-situ reaction of nitrogen-protected iminodiacetic acid using EDCl to form anhydrous iminodiacetic acid and reacting the anhydrous iminodiacetic acid with amines; (2) reacting the resulting compound of the step (1) with 1-(4-chlorobenzhydryl) piperazine; (3) removing a nitrogen protecting group using hydrochloric acid and dioxane; and (4) coupling carboxylic acid to the resulting compound of the step (3).</p> |
