1034606-35-3Relevant academic research and scientific papers
Synthesis and in vivo evaluation of cyclic diaminopropane BACE-1 inhibitors
Thompson, Lorin A.,Shi, Jianliang,Decicco, Carl P.,Tebben, Andrew J.,Olson, Richard E.,Boy, Kenneth M.,Guernon, Jason M.,Good, Andrew C.,Liauw, Ann,Zheng, Changsheng,Copeland, Robert A.,Combs, Andrew P.,Trainor, George L.,Camac, Daniel M.,Muckelbauer, Jodi K.,Lentz, Kimberley A.,Grace, James E.,Burton, Catherine R.,Toyn, Jeremy H.,Barten, Donna M.,Marcinkeviciene, Jovita,Meredith, Jere E.,Albright, Charles F.,MacOr, John E.
, p. 6909 - 6915 (2011/12/22)
The synthesis, evaluation, and structure-activity relationships of a set of related constrained diaminopropane inhibitors of BACE-1 are described. The full in vivo profile of an optimized inhibitor in both normal and P-gp deficient mice is compared with data generated in normal rats.
Monosubstituted γ-lactam and conformationally constrained 1,3-diaminopropan-2-ol transition-state isostere inhibitors of β-secretase (BACE)
Boy, Kenneth M.,Guernon, Jason M.,Shi, Jianliang,Toyn, Jeremy H.,Meredith, Jere E.,Barten, Donna M.,Burton, Catherine R.,Albright, Charles F.,Marcinkeviciene, Jovita,Good, Andrew C.,Tebben, Andrew J.,Muckelbauer, Jodi K.,Camac, Daniel M.,Lentz, Kimberley A.,Bronson, Joanne J.,Olson, Richard E.,MacOr, John E.,Thompson III, Lorin A.
, p. 6916 - 6924 (2011/12/22)
The synthesis, evaluation, and structure-activity relationships of a class of γ-lactam 1,3-diaminopropan-2-ol transition-state isostere inhibitors of BACE are discussed. Two strategies for optimizing lead compound 1a are presented. Reducing the overall size of the inhibitors resulted in the identification of γ-lactam 1i, whereas the introduction of conformational constraint on the prime-side of the inhibitor generated compounds such as the 3-hydroxypyrrolidine inhibitor 28n. The full in vivo profile of 1i in rats and 28n in Tg 2576 mice is presented.
Substituted Tetrahydroisoquinolines as Beta-secretase Inhibitors
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Page/Page column 27-28, (2008/12/06)
There is provided a series of tetrahydroisoquinoline diaminopropane compounds of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R, R8 and R9 are as defined herein, their pharmaceutical compositi
