| 15186838 |
Kam YL, Rhee SJ, Choo HY: Solution-phase combinatorial synthesis of nonpeptide bradykinin antagonists. Bioorg Med Chem. 2004 Jul 1;12(13):3543-52.
We describe the solution-phase combinatorial synthesis and pharmacological effect of fifty N,N (')-substituted-N"-1-(4-chlorobenzhydryl) piperazine iminodiacetic acid triamide derivatives as nonpeptide B2 antagonists. The synthesized compounds were tested for their antibradykinin activity by utilizing guinea-pig ileum smooth muscle. Most of the compounds showed antagonistic effects on bradykinin induced contraction. N-acetyl-N (')-(4-methylbenzyl)-N"-1-(4-chlorobenzhydryl) piperazine iminodiacetic acid triamide (A3B1C1) showed the 46% inhibition at 100nM. |
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