Fragment-based discovery and optimization of BACE1 inhibitors

Bioorganic & Medicinal Chemistry Letters
James MaddenT Hesterkamp

Abstract

A novel series of 2-aminobenzimidazole inhibitors of BACE1 has been discovered using fragment-based drug discovery (FBDD) techniques. The rapid optimization of these inhibitors using structure-guided medicinal chemistry is discussed.

References

Nov 29, 1996·Science·S B ShukerS W Fesik
Apr 9, 2008·Current Alzheimer Research·Arun K GhoshJordan Tang
Oct 6, 2009·Biochemistry·Robert GodemannJohn Kemp

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Citations

May 4, 2013·Journal of Computer-aided Molecular Design·José L DomínguezFredy Sussman
Jun 16, 2012·Biochemistry·Duncan E ScottChris Abell
Nov 7, 2012·Journal of Medicinal Chemistry·Tobias GinmanFredrik Rahm
Dec 24, 2011·Acta Crystallographica. Section D, Biological Crystallography·Yechun XuJoel L Sussman
Mar 4, 2014·Analytical Chemistry·Elena Pérez-RuizMenno W J Prins
Jun 6, 2014·ACS Medicinal Chemistry Letters·Jenny ViklundFredrik Rahm
Feb 27, 2014·Journal of Chemical Information and Modeling·Adrián KalásziTímea Polgár
Apr 10, 2013·Expert Opinion on Drug Discovery·Yoshio Hamada, Yoshiaki Kiso
May 21, 2013·Current Opinion in Chemical Biology·Andrew Stamford, Corey Strickland
Apr 7, 2012·Trends in Pharmacological Sciences·Zhaoning Zhu
Apr 21, 2016·ACS Medicinal Chemistry Letters·Hakan Gunaydin, Michael D Bartberger
Nov 11, 2017·Chemistry : a European Journal·Haixia WangHaiming Guo
Jan 6, 2018·Journal of Biomolecular Structure & Dynamics·Lucas J GutiérrezRicardo D Enriz
Dec 13, 2018·ACS Chemical Neuroscience·Hangchen HuYechun Xu
Oct 1, 2021·Journal of Medicinal Chemistry·Murugaiah A M Subbaiah, Nicholas A Meanwell

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