Design of inhibitors of amyloid beta aggregation and BACE1 for conquering Alzheimer's disease

2017 Fiscal Year Final Research Report

• Project/Area Number: 26460163
• Research Category: Grant-in-Aid for Scientific Research (C)
• Allocation Type: Multi-year Fund
• Section: 一般
• Research Field: Drug development chemistry
• Research Institution: Konan University (2016-2017); Kobe Pharmaceutical University (2014-2015)
• Principal Investigator: HAMADA Yoshio 甲南大学, フロンティアサイエンス研究科, 特別研究員 (70424968)
• Project Period (FY): 2014-04-01 – 2018-03-31
• Keywords: アルツハイマー病 / BACE1 / β-セクレターゼ / アミロイドβ / 凝集阻害剤

Outline of Final Research Achievements

The increase of dementia patients is a big issue for Japan as it faces a rapidly against society. To conquer Alzheimer's disease, this reaearch aimed the development of inhibitors of amyloid beta aggregation and BACE1. We designed and synthesized a series of small-sized BACE1 inhibitors with a thiadiazole moiety. These compounds with improved membrane permeability appear to have promise as drug candidates. And we synthesized aggregation inhibitors. These aggregation inhibitors could recognized a specific Abeta conformer, and are expected to use a research tool for pathogenic mechanism analysis.

Free Research Field

創薬化学