Discovery of Extremely Selective Fused Pyridine-Derived β-Site Amyloid Precursor Protein-Cleaving Enzyme (BACE1) Inhibitors with High In Vivo Efficacy through 10s Loop Interactions-Reference-Cited by-同舟云学术

Discovery of Extremely Selective Fused Pyridine-Derived β-Site Amyloid Precursor Protein-Cleaving Enzyme (BACE1) Inhibitors with High In Vivo Efficacy through 10s Loop Interactions

Published:2021-09-23 Issue:19 Volume:64 Page:14165-14174
ISSN:0022-2623
Container-title:Journal of Medicinal Chemistry
language:en
Short-container-title:J. Med. Chem.

Author:

Ueno Tatsuhiko¹,Matsuoka Eriko¹,Asada Naoya¹,Yamamoto Shiho¹^ORCID,Kanegawa Naoki²,Ito Mana³,Ito Hisanori³,Moechars Diederik⁴,Rombouts Frederik J. R.⁵^ORCID,Gijsen Harrie J. M.⁵^ORCID,Kusakabe Ken-ichi¹^ORCID

Affiliation:

1. Laboratory for Medicinal Chemistry Research, Shionogi Pharmaceutical Research Center, 1-1 Futaba-cho 3-chome, Toyonaka, Osaka 561-0825, Japan

2. Laboratory for Drug Discovery & Development, Shionogi Pharmaceutical Research Center, 1-1 Futaba-cho 3-chome, Toyonaka, Osaka 561-0825, Japan

3. Laboratory for Drug Discovery & Disease Research, Shionogi Pharmaceutical Research Center, 1-1 Futaba-cho 3-chome, Toyonaka, Osaka 561-0825, Japan

4. Neuroscience, Janssen Research & Development, Turnhoutseweg 30, B-2340 Beerse, Belgium

5. Discovery Sciences, Janssen Research & Development, Turnhoutseweg 30, B-2340 Beerse, Belgium

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

Link

https://pubs.acs.org/doi/pdf/10.1021/acs.jmedchem.1c00359

Reference41 articles.

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3. Targeting the β secretase BACE1 for Alzheimer's disease therapy

4. Discovery of the 3-Imino-1,2,4-thiadiazinane 1,1-Dioxide Derivative Verubecestat (MK-8931)–A β-Site Amyloid Precursor Protein Cleaving Enzyme 1 Inhibitor for the Treatment of Alzheimer’s Disease

5. The BACE1 inhibitor verubecestat (MK-8931) reduces CNS β-amyloid in animal models and in Alzheimer’s disease patients

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