Hydroxyethylamine-based inhibitors of BACE1: P1-P3 macrocyclization can improve potency, selectivity, and cell activity

Bioorganic and Medicinal Chemistry Letters

Volumn 23, Issue 15, 2013, Pages 4459-4464

  Pennington, Lewis D ^a   Whittington, Douglas A ^a   Bartberger, Michael D ^a   Jordan, Steven R ^a   Monenschein, Holger ^b   Nguyen, Thomas T ^a   Yang, Bryant H ^a   Xue, Qiufen M ^a   Vounatsos, Filisaty ^a   Wahl, Robert C ^a   Chen, Kui ^a   Wood, Stephen ^a   Citron, Martin ^c   Patel, Vinod F ^d   Hitchcock, Stephen A ^b   Zhong, Wenge ^a  

^a AMGEN INC   (United States)

^b TAKEDA PHARMACEUTICALS   (United States)

^c ELI LILLY AND COMPANY   (United States)

^d Sanofi Aventis   (United States)

Author keywords

Secretase; Alzheimer's disease; BACE1 inhibitor; Conformational constraint; Macrocycle

Indexed keywords

AMYLOID BETA PROTEIN; BETA SECRETASE 1; BETA SECRETASE INHIBITOR; CATHEPSIN D; ETHYLAMINE; HYDROXYETHYLAMINE; UNCLASSIFIED DRUG;

ARTICLE; CRYSTAL STRUCTURE; CYCLIZATION; DRUG ACTIVITY; DRUG CONFORMATION; DRUG POTENCY; DRUG SELECTIVITY; HUMAN; HUMAN CELL; MACROCYCLIZATION; X RAY CRYSTALLOGRAPHY;

AMYLOID BETA-PEPTIDES; AMYLOID BETA-PROTEIN PRECURSOR; AMYLOID PRECURSOR PROTEIN SECRETASES; ASPARTIC ACID ENDOPEPTIDASES; BINDING SITES; CATHEPSIN D; CRYSTALLOGRAPHY, X-RAY; ETHYLAMINES; HEK293 CELLS; HUMANS; MACROCYCLIC COMPOUNDS; PROTEIN BINDING; PROTEIN STRUCTURE, TERTIARY;

EID: 84879685323     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2013.05.028     Document Type: Article

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