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

Yoo Lim Kam; Hee Kyung Rhee; Hwa Jung Kim; Seung Keun Back; Heung Sik Na; Hea Young Park Choo

doi:10.1016/j.bmc.2010.01.050

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

Yoo Lim Kam, Hee Kyung Rhee, Hwa Jung Kim, Seung Keun Back, Heung Sik Na, Hea Young Park Choo

Research output: Contribution to journal › Article › peer-review

4 Scopus citations

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.

Original language	English
Pages (from-to)	2327-2336
Number of pages	10
Journal	Bioorganic and Medicinal Chemistry
Volume	18
Issue number	6
DOIs	https://doi.org/10.1016/j.bmc.2010.01.050
State	Published - 15 Mar 2010

Keywords

Allodynia
Antibradykinin agents
Formalin test

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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.",

keywords = "Allodynia, Antibradykinin agents, Formalin test",

author = "Kam, \{Yoo Lim\} and Rhee, \{Hee Kyung\} and Kim, \{Hwa Jung\} and Back, \{Seung Keun\} and Na, \{Heung Sik\} and Choo, \{Hea Young Park\}",

year = "2010",

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doi = "10.1016/j.bmc.2010.01.050",

language = "English",

volume = "18",

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journal = "Bioorganic and Medicinal Chemistry",

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T1 - Synthesis and bradykinin inhibitory activity of novel non-peptide compounds, and evaluation of in vivo analgesic activity

AU - Kam, Yoo Lim

AU - Rhee, Hee Kyung

AU - Kim, Hwa Jung

AU - Back, Seung Keun

AU - Na, Heung Sik

AU - Choo, Hea Young Park

PY - 2010/3/15

Y1 - 2010/3/15

N2 - 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.

AB - 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.

KW - Allodynia

KW - Antibradykinin agents

KW - Formalin test

UR - https://www.scopus.com/pages/publications/77649238323

U2 - 10.1016/j.bmc.2010.01.050

DO - 10.1016/j.bmc.2010.01.050

M3 - Article

C2 - 20189403

AN - SCOPUS:77649238323

SN - 0968-0896

VL - 18

SP - 2327

EP - 2336

JO - Bioorganic and Medicinal Chemistry

JF - Bioorganic and Medicinal Chemistry

IS - 6

ER -

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

Abstract

Keywords

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