116622-38-9Relevant 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.
Antihypertensive 5-amino-4-hydroxyvaleryl derivatives substituted by sulphur-containing groups
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, (2008/06/13)
Compounds of the formula STR1 in which R1 represents acyl substituted by a thio, sulphinyl or sulphonyl group, A represents an optionally N-alkylated α-amino acid residue that is bonded N-terminally to R1 and C-terminally to the grou