Syntheses of NAMDA derivatives inhibiting NO production in BV-2 cells stimulated with lipopolysaccharide

Jai Seo, Ekaruth Srisook, Jin Son Hyo, Onyou Hwang, Young Nam Cha, Yoon Chi Dae

Research output: Contribution to journalArticle

10 Scopus citations

Abstract

Sixteen derivatives of N-acetyl-3-O-methyldopamine (NAMDA), an inhibitor of BH4 synthesis, were designed and synthesized. The ability of these derivatives to inhibit NO and BH4 production by lipopolysaccharide- stimulated BV-2 microglial cells was determined. While NAMDA at 100 μM inhibited NO and BH4 production by only about 20%, its catecholamide 8, indole 23 derivative, 13, and N-acetyl tetrahydroisoquinoline 25 inhibited the NO production by >50% at the same concentration. In particular, 13 and 25 inhibited both NO and BH4 production to similar degrees, which suggested that these compounds might inhibit NO production by blocking BH 4-dependent dimerization of the newly synthesized iNOS monomer.

Original languageEnglish (US)
Pages (from-to)3369-3373
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume15
Issue number14
DOIs
StatePublished - Jul 15 2005
Externally publishedYes

Keywords

  • Inhibition of NO
  • Inhibition of tetrahydrobiopterin
  • NAMDA
  • Nitric oxide
  • Nitric oxide synthase

ASJC Scopus subject areas

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

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