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Solution-phase combinatorial synthesis of nonpeptide bradykinin antagonists

Title
Solution-phase combinatorial synthesis of nonpeptide bradykinin antagonists
Authors
Kam Y.L.Rhee S.-J.Choo H.-Y.P.
Ewha Authors
박혜영
SCOPUS Author ID
박혜영scopus
Issue Date
2004
Journal Title
Bioorganic and Medicinal Chemistry
ISSN
0968-0896JCR Link
Citation
Bioorganic and Medicinal Chemistry vol. 12, no. 13, pp. 3543 - 3552
Indexed
SCI; SCIE; SCOPUS WOS scopus
Document Type
Article
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. © 2004 Elsevier Ltd. All rights reserved.
DOI
10.1016/j.bmc.2004.04.031
Appears in Collections:
약학대학 > 약학과 > Journal papers
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