Bioorganic & Medicinal Chemistry Letters 28 (2018) 1111–1115 Contents lists available at ScienceDirect Bioorganic & Medicinal Chemistry Letters journal homepage: www.elsevier.com/locate/bmcl Diastereoselective synthesis of fused cyclopropyl-3-amino-2,4-oxazine b-amyloid cleaving enzyme (BACE) inhibitors and their biological evaluation a,⇑ b a c,e a Jonathan D. Low , Michael D. Bartberger , Yuan Cheng , Doug Whittington , Quifen Xue , d a a,⇑ Stephen Wood , Jennifer R. Allen , Ana E. Minatti Department of Medicinal Chemistry, Amgen Inc., One Amgen Center Drive, Thousand Oaks, CA 91320, USA Department of Molecular Engineering, Amgen Inc., One Amgen Center Drive, Thousand Oaks, CA 91320, USA Department of Molecular Engineering, Amgen Inc., 360 Binney Street, Cambridge, MA 02142, USA Department of Neuroscience, Amgen Inc., One Amgen Center Drive, Thousand Oaks, CA 91320, USA article i nfo abstract Article history: The diastereoselective synthesis and structure activity relationship (SAR) of a series of fused cyclopropyl- Received 3 January 2018 3-amino-2,4-oxazine (2-oxa-4-azabicyclo[4.1.0]hept-3-en-3-amine)-containing BACE inhibitors is Revised 24 January 2018 described. Through these efforts compound 2 was identiﬁed as a potent (cell IC = 15 nM) BACE inhibitor Accepted 26 January 2018 with acceptable ADME properties. When tested in vivo, compound 2 demonstrated a signiﬁcant reduc- Available online 1
Bioorganic & Medicinal Chemistry Letters – Elsevier
Published: Apr 1, 2018
It’s your single place to instantly
discover and read the research
that matters to you.
Enjoy affordable access to
over 18 million articles from more than
15,000 peer-reviewed journals.
All for just $49/month
Query the DeepDyve database, plus search all of PubMed and Google Scholar seamlessly
Save any article or search result from DeepDyve, PubMed, and Google Scholar... all in one place.
Get unlimited, online access to over 18 million full-text articles from more than 15,000 scientific journals.
Read from thousands of the leading scholarly journals from SpringerNature, Elsevier, Wiley-Blackwell, Oxford University Press and more.
All the latest content is available, no embargo periods.
“Hi guys, I cannot tell you how much I love this resource. Incredible. I really believe you've hit the nail on the head with this site in regards to solving the research-purchase issue.”Daniel C.
“Whoa! It’s like Spotify but for academic articles.”@Phil_Robichaud
“I must say, @deepdyve is a fabulous solution to the independent researcher's problem of #access to #information.”@deepthiw
“My last article couldn't be possible without the platform @deepdyve that makes journal papers cheaper.”@JoseServera