Development of 2-aminooxazoline 3-azaxanthenes as orally efficacious β-secretase inhibitors for the potential treatment of Alzheimer’s disease
[Display omitted] The β-site amyloid precursor protein (APP) cleaving enzyme 1 (BACE1) is one of the most hotly pursued targets for the treatment of Alzheimer’s disease. We used a structure- and property-based drug design approach to identify 2-aminooxazoline 3-azaxanthenes as potent BACE1 inhibitor...
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| Published in | Bioorganic & medicinal chemistry letters Vol. 25; no. 4; pp. 767 - 774 |
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| Main Authors | , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , |
| Format | Journal Article |
| Language | English |
| Published |
OXFORD
Elsevier Ltd
15.02.2015
Elsevier |
| Subjects | |
| Online Access | Get full text |
| ISSN | 0960-894X 1464-3405 1464-3405 |
| DOI | 10.1016/j.bmcl.2014.12.092 |
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| Abstract | [Display omitted]
The β-site amyloid precursor protein (APP) cleaving enzyme 1 (BACE1) is one of the most hotly pursued targets for the treatment of Alzheimer’s disease. We used a structure- and property-based drug design approach to identify 2-aminooxazoline 3-azaxanthenes as potent BACE1 inhibitors which significantly reduced CSF and brain Aβ levels in a rat pharmacodynamic model. Compared to the initial lead 2, compound 28 exhibited reduced potential for QTc prolongation in a non-human primate cardiovascular safety model. |
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| AbstractList | The beta-site amyloid precursor protein (APP) cleaving enzyme 1 (BACE1) is one of the most hotly pursued targets for the treatment of Alzheimer's disease. We used a structure-and property-based drug design approach to identify 2-aminooxazoline 3-azaxanthenes as potent BACE1 inhibitors which significantly reduced CSF and brain Ab levels in a rat pharmacodynamic model. Compared to the initial lead 2, compound 28 exhibited reduced potential for QTc prolongation in a non-human primate cardiovascular safety model. (C) 2015 Elsevier Ltd. All rights reserved. The β-site amyloid precursor protein (APP) cleaving enzyme 1 (BACE1) is one of the most hotly pursued targets for the treatment of Alzheimer's disease. We used a structure- and property-based drug design approach to identify 2-aminooxazoline 3-azaxanthenes as potent BACE1 inhibitors which significantly reduced CSF and brain Aβ levels in a rat pharmacodynamic model. Compared to the initial lead 2, compound 28 exhibited reduced potential for QTc prolongation in a non-human primate cardiovascular safety model.The β-site amyloid precursor protein (APP) cleaving enzyme 1 (BACE1) is one of the most hotly pursued targets for the treatment of Alzheimer's disease. We used a structure- and property-based drug design approach to identify 2-aminooxazoline 3-azaxanthenes as potent BACE1 inhibitors which significantly reduced CSF and brain Aβ levels in a rat pharmacodynamic model. Compared to the initial lead 2, compound 28 exhibited reduced potential for QTc prolongation in a non-human primate cardiovascular safety model. [Display omitted] The β-site amyloid precursor protein (APP) cleaving enzyme 1 (BACE1) is one of the most hotly pursued targets for the treatment of Alzheimer’s disease. We used a structure- and property-based drug design approach to identify 2-aminooxazoline 3-azaxanthenes as potent BACE1 inhibitors which significantly reduced CSF and brain Aβ levels in a rat pharmacodynamic model. Compared to the initial lead 2, compound 28 exhibited reduced potential for QTc prolongation in a non-human primate cardiovascular safety model. The beta -site amyloid precursor protein (APP) cleaving enzyme 1 (BACE1) is one of the most hotly pursued targets for the treatment of Alzheimer's disease. We used a structure- and property-based drug design approach to identify 2-aminooxazoline 3-azaxanthenes as potent BACE1 inhibitors which significantly reduced CSF and brain A beta levels in a rat pharmacodynamic model. Compared to the initial lead 2, compound 28 exhibited reduced potential for QTc prolongation in a non-human primate cardiovascular safety model. The β-site amyloid precursor protein (APP) cleaving enzyme 1 (BACE1) is one of the most hotly pursued targets for the treatment of Alzheimer's disease. We used a structure- and property-based drug design approach to identify 2-aminooxazoline 3-azaxanthenes as potent BACE1 inhibitors which significantly reduced CSF and brain Aβ levels in a rat pharmacodynamic model. Compared to the initial lead 2, compound 28 exhibited reduced potential for QTc prolongation in a non-human primate cardiovascular safety model. |
| Author | Cheng, Yuan Marx, Isaac Wen, Paul H. Whittington, Douglas A. Cheng, Alan C. Hickman, Dean Yuan, Chester Everds, Nancy E. Zhong, Wenge Bartberger, Michael D. Gore, Vijay Powers, Timothy S. Chen, Kui Ma, Vu Dunn, Robert T. Xue, May Patel, Vinod F. Hitchcock, Stephen A. Amegadzie, Albert Qian, Wenyuan Vonderfecht, Steven L. Brown, James Epstein, Oleg Vargas, Hugo M. Human, Jason White, Ryan D. Fremeau, Robert T. Liu, Qingyian Judd, Ted C. Minatti, Ana E. Wood, Stephen Lopez, Patricia Weiss, Matthew M. Kreiman, Charles Chen, Jian Jeffrey Dineen, Thomas A. Werner, Jonathan A. |
| Author_xml | – sequence: 1 givenname: Jian Jeffrey surname: Chen fullname: Chen, Jian Jeffrey email: jianc@amgen.com organization: Department of Medicinal Chemistry, Amgen Inc., One Amgen Center Drive, Thousand Oaks, CA 91320, USA – sequence: 2 givenname: Qingyian surname: Liu fullname: Liu, Qingyian organization: Department of Medicinal Chemistry, Amgen Inc., One Amgen Center Drive, Thousand Oaks, CA 91320, USA – sequence: 3 givenname: Chester surname: Yuan fullname: Yuan, Chester organization: Department of Medicinal Chemistry, Amgen Inc., One Amgen Center Drive, Thousand Oaks, CA 91320, USA – sequence: 4 givenname: Vijay surname: Gore fullname: Gore, Vijay organization: Department of Medicinal Chemistry, Amgen Inc., One Amgen Center Drive, Thousand Oaks, CA 91320, USA – sequence: 5 givenname: Patricia surname: Lopez fullname: Lopez, Patricia organization: Department of Medicinal Chemistry, Amgen Inc., One Amgen Center Drive, Thousand Oaks, CA 91320, USA – sequence: 6 givenname: Vu surname: Ma fullname: Ma, Vu organization: Department of Medicinal Chemistry, Amgen Inc., One Amgen Center Drive, Thousand Oaks, CA 91320, USA – sequence: 7 givenname: Albert surname: Amegadzie fullname: Amegadzie, Albert organization: Department of Medicinal Chemistry, Amgen Inc., One Amgen Center Drive, Thousand Oaks, CA 91320, USA – sequence: 8 givenname: Wenyuan surname: Qian fullname: Qian, Wenyuan organization: Department of Medicinal Chemistry, Amgen Inc., One Amgen Center Drive, Thousand Oaks, CA 91320, USA – sequence: 9 givenname: Ted C. surname: Judd fullname: Judd, Ted C. organization: Department of Medicinal Chemistry, Amgen Inc., One Amgen Center Drive, Thousand Oaks, CA 91320, USA – sequence: 10 givenname: Ana E. surname: Minatti fullname: Minatti, Ana E. organization: Department of Medicinal Chemistry, Amgen Inc., One Amgen Center Drive, Thousand Oaks, CA 91320, USA – sequence: 11 givenname: James surname: Brown fullname: Brown, James organization: Department of Medicinal Chemistry, Amgen Inc., One Amgen Center Drive, Thousand Oaks, CA 91320, USA – sequence: 12 givenname: Yuan surname: Cheng fullname: Cheng, Yuan organization: Department of Medicinal Chemistry, Amgen Inc., One Amgen Center Drive, Thousand Oaks, CA 91320, USA – sequence: 13 givenname: May surname: Xue fullname: Xue, May organization: Department of Medicinal Chemistry, Amgen Inc., One Amgen Center Drive, Thousand Oaks, CA 91320, USA – sequence: 14 givenname: Wenge surname: Zhong fullname: Zhong, Wenge organization: Department of Medicinal Chemistry, Amgen Inc., One Amgen Center Drive, Thousand Oaks, CA 91320, USA – sequence: 15 givenname: Thomas A. surname: Dineen fullname: Dineen, Thomas A. organization: Department of Medicinal Chemistry, Amgen Inc., 360 Binney Street, Cambridge, MA 02142, USA – sequence: 16 givenname: Oleg surname: Epstein fullname: Epstein, Oleg organization: Department of Medicinal Chemistry, Amgen Inc., 360 Binney Street, Cambridge, MA 02142, USA – sequence: 17 givenname: Jason surname: Human fullname: Human, Jason organization: Department of Medicinal Chemistry, Amgen Inc., 360 Binney Street, Cambridge, MA 02142, USA – sequence: 18 givenname: Charles surname: Kreiman fullname: Kreiman, Charles organization: Department of Medicinal Chemistry, Amgen Inc., 360 Binney Street, Cambridge, MA 02142, USA – sequence: 19 givenname: Isaac surname: Marx fullname: Marx, Isaac organization: Department of Medicinal Chemistry, Amgen Inc., 360 Binney Street, Cambridge, MA 02142, USA – sequence: 20 givenname: Matthew M. surname: Weiss fullname: Weiss, Matthew M. organization: Department of Medicinal Chemistry, Amgen Inc., 360 Binney Street, Cambridge, MA 02142, USA – sequence: 21 givenname: Stephen A. surname: Hitchcock fullname: Hitchcock, Stephen A. organization: Department of Medicinal Chemistry, Amgen Inc., One Amgen Center Drive, Thousand Oaks, CA 91320, USA – sequence: 22 givenname: Timothy S. surname: Powers fullname: Powers, Timothy S. organization: Department of Medicinal Chemistry, Amgen Inc., One Amgen Center Drive, Thousand Oaks, CA 91320, USA – sequence: 23 givenname: Kui surname: Chen fullname: Chen, Kui organization: Department of HTS and Molecular Pharmacology, Amgen Inc., One Amgen Center Drive, Thousand Oaks, CA 91320, USA – sequence: 24 givenname: Paul H. surname: Wen fullname: Wen, Paul H. organization: Department of Neuroscience, Amgen Inc., One Amgen Center Drive, Thousand Oaks, CA 91320, USA – sequence: 25 givenname: Douglas A. surname: Whittington fullname: Whittington, Douglas A. organization: Department of Molecular Structure, Amgen Inc., 360 Binney Street, Cambridge, MA 02142, USA – sequence: 26 givenname: Alan C. surname: Cheng fullname: Cheng, Alan C. organization: Department of Molecular Structure, Amgen Inc., 360 Binney Street, Cambridge, MA 02142, USA – sequence: 27 givenname: Michael D. surname: Bartberger fullname: Bartberger, Michael D. organization: Department of Molecular Structure, Amgen Inc., One Amgen Center Drive, Thousand Oaks, CA 91320, USA – sequence: 28 givenname: Dean surname: Hickman fullname: Hickman, Dean organization: Department of Pharmacokinetics and Drug Metabolism, Amgen Inc., One Amgen Center Drive, Thousand Oaks, CA 91320, USA – sequence: 29 givenname: Jonathan A. surname: Werner fullname: Werner, Jonathan A. organization: Comparative Biology and Safety Sciences, Amgen Inc., One Amgen Center Drive, Thousand Oaks, CA 91320, USA – sequence: 30 givenname: Hugo M. surname: Vargas fullname: Vargas, Hugo M. organization: Comparative Biology and Safety Sciences, Amgen Inc., One Amgen Center Drive, Thousand Oaks, CA 91320, USA – sequence: 31 givenname: Nancy E. surname: Everds fullname: Everds, Nancy E. organization: Comparative Biology and Safety Sciences, Amgen Inc., One Amgen Center Drive, Thousand Oaks, CA 91320, USA – sequence: 32 givenname: Steven L. surname: Vonderfecht fullname: Vonderfecht, Steven L. organization: Comparative Biology and Safety Sciences, Amgen Inc., One Amgen Center Drive, Thousand Oaks, CA 91320, USA – sequence: 33 givenname: Robert T. surname: Dunn fullname: Dunn, Robert T. organization: Comparative Biology and Safety Sciences, Amgen Inc., One Amgen Center Drive, Thousand Oaks, CA 91320, USA – sequence: 34 givenname: Stephen surname: Wood fullname: Wood, Stephen organization: Department of Neuroscience, Amgen Inc., One Amgen Center Drive, Thousand Oaks, CA 91320, USA – sequence: 35 givenname: Robert T. surname: Fremeau fullname: Fremeau, Robert T. organization: Department of Neuroscience, Amgen Inc., One Amgen Center Drive, Thousand Oaks, CA 91320, USA – sequence: 36 givenname: Ryan D. surname: White fullname: White, Ryan D. organization: Department of Medicinal Chemistry, Amgen Inc., 360 Binney Street, Cambridge, MA 02142, USA – sequence: 37 givenname: Vinod F. surname: Patel fullname: Patel, Vinod F. organization: Department of Medicinal Chemistry, Amgen Inc., 360 Binney Street, Cambridge, MA 02142, USA |
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| Keywords | Alzheimer’s disease (AD) Aminooxazoline 3-Azaxanthene Amyloid β-Secretase (BACE1) Xanthene Aβ peptides ENZYME BACE1 INHIBITORS DESIGN SERIES HYPOTHESIS Alzheimer's disease (AD) AMYLOID PRECURSOR PROTEIN beta-Secretase (BACE1) A beta peptides |
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The β-site amyloid precursor protein (APP) cleaving enzyme 1 (BACE1) is one of the most hotly pursued targets for the treatment of... The beta-site amyloid precursor protein (APP) cleaving enzyme 1 (BACE1) is one of the most hotly pursued targets for the treatment of Alzheimer's disease. We... The β-site amyloid precursor protein (APP) cleaving enzyme 1 (BACE1) is one of the most hotly pursued targets for the treatment of Alzheimer's disease. We used... The beta -site amyloid precursor protein (APP) cleaving enzyme 1 (BACE1) is one of the most hotly pursued targets for the treatment of Alzheimer's disease. We... |
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| SubjectTerms | 3-Azaxanthene Alzheimer Disease - drug therapy Alzheimer’s disease (AD) Aminooxazoline Amyloid Amyloid Precursor Protein Secretases - antagonists & inhibitors Animals Aspartic Acid Endopeptidases - antagonists & inhibitors Aβ peptides Cell Line Chemistry Chemistry, Medicinal Chemistry, Organic HEK293 Cells Humans Life Sciences & Biomedicine Pharmacology & Pharmacy Physical Sciences Protease Inhibitors - chemical synthesis Protease Inhibitors - chemistry Protease Inhibitors - pharmacology Rats Science & Technology Xanthene Xanthenes - chemical synthesis Xanthenes - chemistry Xanthenes - pharmacology β-Secretase (BACE1) |
| Title | Development of 2-aminooxazoline 3-azaxanthenes as orally efficacious β-secretase inhibitors for the potential treatment of Alzheimer’s disease |
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