4′-Methyl-4,5′-bithiazole-based correctors of defective ΔF508-CFTR cellular processing

Choong Leol Yoo, Gui Jun Yu, Baoxue Yang, Lori I. Robins, A. S. Verkman, Mark J. Kurth

Research output: Contribution to journalArticle

37 Scopus citations

Abstract

The synthesis and ΔF508-CFTR corrector activity of a 148-member methylbithiazole-based library are reported. Synthetic routes were devised and optimized to generate methylbithiazole analogs in four steps. Corrector potency and efficacy were assayed using epithelial cells expressing human ΔF508-CFTR. These structure-activity data establish that the bithiazole substructure plays a critical function; eight novel methylbithiazole correctors were identified with low micromolar potencies.

Original languageEnglish (US)
Pages (from-to)2610-2614
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume18
Issue number8
DOIs
StatePublished - Apr 15 2008

Keywords

  • ΔF508-CFTR correctors
  • Bithiazole
  • Small-molecule library
  • Structure-activity

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology
  • Organic Chemistry
  • Drug Discovery
  • Pharmaceutical Science
  • Medicine(all)

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