Therapeutic and pharmacokinetic characterizations of an anti-amyloidogenic bis-styrylbenzene derivative for Alzheimer's disease treatment

Seong Rim Byeon, Hyunjin Vincent Kim, Mijin Jeon, Young Gil Ahn, Maeng Sup Kim, Jae Yang Kong, Hye Yun Kim, Young Soo Kim, Dong Jin Kim

Research output: Contribution to journalArticle

5 Citations (Scopus)

Abstract

Alzheimer's disease drug discovery regarding exploration into the molecules and processes has focused on the intrinsic causes of the brain disorder correlated with the accumulation of amyloid-β. An anti-amyloidogenic bis-styrylbenzene derivative, KMS80013, showed excellent oral bioavailability (F = 46.2%), facilitated brain penetration (26%, iv) in mouse and target specific in vivo efficacy in acute AD mouse model attenuating the cognitive deficiency in Y-maze test. Acute toxicity (LD50 >2000 mg/kg) and hERG channel inhibition (14% at 10 μM) results indicated safety of KMS80013.

Original languageEnglish
Pages (from-to)3467-3469
Number of pages3
JournalBioorganic and Medicinal Chemistry Letters
Volume23
Issue number11
DOIs
Publication statusPublished - 2013 Jun 1

All Science Journal Classification (ASJC) codes

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

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