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, H. Y P Choo

Research output: Contribution to journalArticle

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

Fingerprint

Diamide
Neuralgia
Bradykinin
Ileum
Smooth Muscle
Analgesics
Muscle
Rats
Guinea Pigs

Keywords

  • Allodynia
  • Antibradykinin agents
  • Formalin test

ASJC Scopus subject areas

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

Cite this

Synthesis and bradykinin inhibitory activity of novel non-peptide compounds, and evaluation of in vivo analgesic activity. / Kam, Yoo Lim; Rhee, Hee Kyung; Kim, Hwa Jung; Back, Seung Keun; Na, Heung Sik; Choo, H. Y P.

In: Bioorganic and Medicinal Chemistry, Vol. 18, No. 6, 15.03.2010, p. 2327-2336.

Research output: Contribution to journalArticle

Kam, Yoo Lim ; Rhee, Hee Kyung ; Kim, Hwa Jung ; Back, Seung Keun ; Na, Heung Sik ; Choo, H. Y P. / Synthesis and bradykinin inhibitory activity of novel non-peptide compounds, and evaluation of in vivo analgesic activity. In: Bioorganic and Medicinal Chemistry. 2010 ; Vol. 18, No. 6. pp. 2327-2336.
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