title: Synthesis and bradykinin inhibitory activity of novel non-peptide compounds, and evaluation of in vivo analgesic activity.
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.
authors.affiliation: School of Pharmacy, Ewha Womans University, Seoul 120-750, Republic of Korea.
authors.forename: Yoo Lim
authors.initials: YL
authors.lastname: Kam
authors.affiliation: Department of Biological Science, Sookmyung Women's University, Seoul 140-742, Republic of Korea.
authors.forename: Hee-Kyung
authors.initials: HK
authors.lastname: Rhee
authors.affiliation: School of Pharmacy, Ewha Womans University, Seoul 120-750, Republic of Korea.
authors.forename: Hwa-Jung
authors.initials: HJ
authors.lastname: Kim
authors.affiliation: Department of Physiology, Korea University College of Medicine, Seoul 136-705, Republic of Korea.
authors.forename: Seung Keun
authors.initials: SK
authors.lastname: Back
authors.affiliation: Department of Physiology, Korea University College of Medicine, Seoul 136-705, Republic of Korea.
authors.forename: Heung Sik
authors.initials: HS
authors.lastname: Na
authors.affiliation: School of Pharmacy, Ewha Womans University, Seoul 120-750, Republic of Korea.
authors.forename: Hea-Young Park
authors.initials: HP
authors.lastname: Choo
mesh_terms: D000700:Analgesics / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D001920:Bradykinin / Q000037:antagonists & inhibitors* / Q000737:chemistry / Q000378:metabolism; D003958:Diamide / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004195:Disease Models, Animal; D006168:Guinea Pigs; D007082:Ileum / Q000187:drug effects; D007249:Inflammation / Q000139:chemically induced / Q000188:drug therapy*; D015394:Molecular Structure; D009130:Muscle, Smooth / Q000187:drug effects; D010146:Pain / Q000139:chemically induced / Q000188:drug therapy*; D051381:Rats; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: D000700:Analgesics; D000893:Anti-Inflammatory Agents; D003958:Diamide; D001920:Bradykinin