Synthesis and bradykinin inhibitory activity of novel non-peptide compounds,and evaluation of in vivo analgesic activity |
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| Authors: | Yoo Lim Kam Hee-Kyung Rhee Hwa-Jung Kim Seung Keun Back Heung Sik Na Hea-Young Park Choo |
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| Affiliation: | 1. School of Pharmacy, Ewha Womans University, Seoul 120-750, Republic of Korea;2. Department of Biological Science, Sookmyung Women’s University, Seoul 140-742, Republic of Korea;3. Department of Physiology, Korea University College of Medicine, Seoul 136-705, Republic of Korea |
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| 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. |
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