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Synthesis and bradykinin inhibitory activity of novel non-peptide compounds, and evaluation of in vivo analgesic activity
- Authors
- Kam, Yoo Lim; Rhee, Hee-Kyung; Kim, Hwa-Jung; Back, Seung Keun; Na, Heung Sik; Choo, Hea-Young Park
- Issue Date
- 15-Mar-2010
- Publisher
- PERGAMON-ELSEVIER SCIENCE LTD
- Keywords
- Antibradykinin agents; Formalin test; Allodynia
- Citation
- BIOORGANIC & MEDICINAL CHEMISTRY, v.18, no.6, pp 2327 - 2336
- Pages
- 10
- Journal Title
- BIOORGANIC & MEDICINAL CHEMISTRY
- Volume
- 18
- Number
- 6
- Start Page
- 2327
- End Page
- 2336
- ISSN
- 0968-0896
1464-3391
- 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. (C) 2010 Published by Elsevier Ltd.
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