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Synthesis and bradykinin inhibitory activity of novel non-peptide compounds, and evaluation of in vivo analgesic activity

Title
Synthesis and bradykinin inhibitory activity of novel non-peptide compounds, and evaluation of in vivo analgesic activity
Authors
Kam Y.L.Rhee H.-K.Kim H.-J.Back S.K.Na H.S.Choo H.-Y.P.
Ewha Authors
박혜영김화정
SCOPUS Author ID
박혜영scopus; 김화정scopus
Issue Date
2010
Journal Title
Bioorganic and Medicinal Chemistry
ISSN
0968-0896JCR Link
Citation
vol. 18, no. 6, pp. 2327 - 2336
Indexed
SCI; SCIE; SCOPUS WOS scopus
Abstract
A series of novel non-peptide diamide compounds was synthesized and evaluated as antibradykinin agents by utilizing guinea-pig ileum smooth muscle. Among the final compounds, (Z)-4-(4-(bis(4-fluorophenyl)methyl)piperazin-1-yl)-4-oxo-N-(4-phenylbutan-2-yl)but-2-enamide showed most favorable bradykinin inhibitory activity and demonstrated analgesic efficacies in the rat models of inflammatory and neuropathic pain. © 2010.
DOI
10.1016/j.bmc.2010.01.050
Appears in Collections:
약학대학 > 약학과 > Journal papers
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