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Solution-phase combinatorial synthesis of nonpeptide bradykinin antagonists
Kam, Yoo-Lim,Rhee, Soo-Jin,P.Choo, Hea-Young 이화여자대학교 약학연구소 2004 藥學硏究論文集 Vol.- No.14
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.