2. Academic Validation
  3. Discovery of an Orally Bioavailable Benzofuran Analogue That Serves as a β-Amyloid Aggregation Inhibitor for the Potential Treatment of Alzheimer's Disease

Discovery of an Orally Bioavailable Benzofuran Analogue That Serves as a β-Amyloid Aggregation Inhibitor for the Potential Treatment of Alzheimer's Disease

  • J Med Chem. 2018 Jan 11;61(1):396-402. doi: 10.1021/acs.jmedchem.7b00844.
Hee-Jin Ha 1 2,  Dong Wook Kang 3,  Hyuk-Min Kim 3,  Jin-Mi Kang 3,  Jihyae Ann 3,  Hyae Jung Hyun 4,  Joon Hwan Lee 4,  Sae Hee Kim 4,  Hee Kim 1,  Kwanghyun Choi 1,  Hyun-Seok Hong 1,  YoungHo Kim 1,  Dong-Gyu Jo 2,  Jiyoun Lee 5,  Jeewoo Lee 3
Affiliations

Affiliations

  • 1 Medifron DBT , Sandanro 349, Danwon-gu, Ansan-si, Gyeonggi-do 15426, Republic of Korea.
  • 2 School of Pharmacy, Sungkyunkwan University , 2066 Seobu-ro, Jangan-gu, Suwon, Gyeonggi-do 16419, Republic of Korea.
  • 3 Laboratory of Medicinal Chemistry, College of Pharmacy, Seoul National University , 1 Gwanak-ro, Gwanak-gu, Seoul 08826, Republic of Korea.
  • 4 Daewoong Pharmaceutical , 72 Dugye-ro, Pogok-eup, Cheoin-gu, Yongin-si, Gyeonggi-do 17028, Republic of Korea.
  • 5 Department of Global Medical Science, Sungshin University , 76 Dobong-ro, Gangbuk-gu, Seoul 01133, Republic of Korea.
PMID: 29161514 DOI: 10.1021/acs.jmedchem.7b00844
Abstract

We developed an orally active and blood-brain-barrier-permeable benzofuran analogue (8, MDR-1339) with potent antiaggregation activity. Compound 8 restored cellular viability from Aβ-induced cytotoxicity but also improved the learning and memory function of AD model mice by reducing the Aβ aggregates in the brains. Given the high bioavailability and brain permeability demonstrated in our pharmacokinetic studies, 8 will provide a novel scaffold for an Aβ-aggregation inhibitor that may offer an alternative treatment for AD.

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