Article

Solution-phase combinatorial synthesis of nonpeptide bradykinin antagonists.

School of Pharmacy, Ewha Womans University, Seoul 120-750, South Korea.
Bioorganic & Medicinal Chemistry (impact factor: 2.92). 08/2004; 12(13):3543-52. DOI:10.1016/j.bmc.2004.04.031 pp.3543-52
Source: PubMed

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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Keywords

46% inhibition
 
antibradykinin activity
 
bradykinin induced contraction
 
compounds
 
nonpeptide B2 antagonists
 
synthesized compounds
 
utilizing guinea-pig ileum smooth muscle
 

Yoo Lim Kam