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 journalArticlepeer-review

4 Citations (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.

Original languageEnglish
Pages (from-to)2327-2336
Number of pages10
JournalBioorganic and Medicinal Chemistry
Volume18
Issue number6
DOIs
Publication statusPublished - 2010 Mar 15

Bibliographical note

Funding Information:
This study was supported in part by the Korea Research foundation (Grants KRF-2004-E00406 and KRF-2005-041-E20291 ) and Grant ( M103KV010015-08K2201-01510 ) from Brain Research Center of the 21st Century Frontier Research Program funded by the Ministry of Education, Science and Technology, the Republic of Korea.

Keywords

  • Allodynia
  • Antibradykinin agents
  • Formalin test

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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