498-96-4Relevant articles and documents
Discovery of potent iminoheterocycle BACE1 inhibitors
Caldwell, John P.,Mazzola, Robert D.,Durkin, James,Chen, Joseph,Chen, Xia,Favreau, Leonard,Kennedy, Matthew,Kuvelkar, Reshma,Lee, Julie,McHugh, Nansie,McKittrick, Brian,Orth, Peter,Stamford, Andrew,Strickland, Corey,Voigt, Johannes,Wang, Liyang,Zhang, Lili,Zhang, Qi,Zhu, Zhaoning
, p. 5455 - 5459 (2015/01/08)
The synthesis of a series of iminoheterocycles and their structure-activity relationships (SAR) as inhibitors of the aspartyl protease BACE1 will be detailed. An effort to access the S3 subsite directly from the S1 subsite initially yielded compounds with sub-micromolar potency. A subset of compounds from this effort unexpectedly occupied a different binding site and displayed excellent BACE1 affinities. Select compounds from this subset acutely lowered Aβ40 levels upon subcutaneous and oral administration to rats.
USE OF NEUROPROTECTIVE COMPOUNDS IN OBTAINING MEDICAMENTS INTENDED FOR THE TREATMENT OF NEURODEGENERATING DISEASES
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, (2009/12/23)
Use of neuroprotective compounds in obtaining medicaments intended for the curative treatment of neurodegenerative disease and/or the prevention of the appearance of disorders ensuing from those diseases.
Inhibitors of GABA uptake. Syntheses and 1H NMR spectroscopic investigations of guvacine, (3RS,4SR)-4-hydroxypiperidine-3-carboxylic acid, and related compounds
Krogsgaard-Larsen,Thyssen,Schaumburg
, p. 327 - 334 (2007/10/04)
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