Aβ Aggregation inhibitors. Part 1: Synthesis and biological activity of phenylazo benzenesulfonamides

Shwu Jiuan Lin, Young Ji Shiao, Chih Wen Chi, Li Ming Yang

Research output: Contribution to journalArticle

22 Citations (Scopus)

Abstract

Phenylazo benzenesulfonamides were designed and synthesized as β-amyloid (Aβ40) fibril assembly inhibitors, and evaluated for inhibition of Aβ40 aggregation and neurotoxicity using rat cortical neurons. Compound 2 (LB-152) was the most potent compound in this study, and the para-NMe2 group on the end of the phenylazo moiety may play an important role in preventing Aβ40 fibril formation. LB-152 provides a new lead for further development of potential β-amyloid aggregation inhibitors to treat AD.

Original languageEnglish
Pages (from-to)1173-1176
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume14
Issue number5
DOIs
Publication statusPublished - Mar 8 2004

Fingerprint

Bioactivity
Amyloid
Agglomeration
Neurons
Rats
benzenesulfonamide
Lead

Keywords

  • Alzheimer's disease
  • Benzenesulfonamide
  • beta-Amyloid
  • Phenylazo

ASJC Scopus subject areas

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

Cite this

Aβ Aggregation inhibitors. Part 1 : Synthesis and biological activity of phenylazo benzenesulfonamides. / Lin, Shwu Jiuan; Shiao, Young Ji; Chi, Chih Wen; Yang, Li Ming.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 14, No. 5, 08.03.2004, p. 1173-1176.

Research output: Contribution to journalArticle

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