917386-29-9Relevant academic research and scientific papers
Acyl guanidine inhibitors of β-secretase (bACE-1): Optimization of a micromolar hit to a nanomolar lead via iterative solid- and solution-phase library synthesis
Gerritz, Samuel W.,Zhai, Weixu,Shi, Shuhao,Zhu, Shirong,Toyn, Jeremy H.,Meredith, Jere E.,Iben, Lawrence G.,Burton, Catherine R.,Albright, Charles F.,Good, Andrew C.,Cook, Lynda S.,Padmanabha, Ramesh,Lentz, Kimberley A.,Sofia, Michael J.,MacOr, John E.,Thompson, Lorin A.,Tebben, Andrew J.,Muckelbauer, Jodi K.,Camac, Daniel M.,Metzler, William,Poss, Michael A.
, p. 9208 - 9223,16 (2020/10/15)
This report describes the discovery and optimization of a BACE-1 inhibitor series containing an unusual acyl guanidine chemotype that was originally synthesized as part of a 6041-membered solid-phase library. The synthesis of multiple follow-up solid- and
Aminoacetamide acyl guanidines as beta-secretase inhibitors
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Page/Page column 49-50, (2008/06/13)
There is provided a series of substituted acyl guanidines of Formula (Ik) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R2, R3, R4, R5, R25, R26 and R27 as defined herein, their pharmaceutical compositions and methods of use. These compounds inhibit the processing of amyloid precursor protein (APP) by β-secretase and, more specifically, inhibit the production of Aβ-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to β-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.
