Solution-phase combinatorial synthesis of nonpeptide bradykinin antagonists
Yoo Lim Kam1, Soo-Jin Rhee, Hea-Young P Choo
1School of Pharmacy, Ewha Womans University, Seoul 120-750, South Korea.
Abstract:
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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