Literature DB >> 17434734

Potent and selective isophthalamide S2 hydroxyethylamine inhibitors of BACE1.

Steven W Kortum1, Timothy E Benson, Michael J Bienkowski, Thomas L Emmons, D Bryan Prince, Donna J Paddock, Alfredo G Tomasselli, Joseph B Moon, Alice LaBorde, Ruth E TenBrink.   

Abstract

The design and synthesis of a novel series of potent BACE1 hydroxyethylamine inhibitors. These inhibitors feature hydrogen bonding substituents at the C-5 position of the isophthalamide ring with improved selectivity over cathepsin D.

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Year:  2007        PMID: 17434734     DOI: 10.1016/j.bmcl.2007.03.096

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  7 in total

Review 1.  beta-Secretase as a therapeutic target for Alzheimer's disease.

Authors:  Arun K Ghosh; Sandra Gemma; Jordan Tang
Journal:  Neurotherapeutics       Date:  2008-07       Impact factor: 7.620

2.  D3R Grand Challenge 4: ligand similarity and MM-GBSA-based pose prediction and affinity ranking for BACE-1 inhibitors.

Authors:  Sukanya Sasmal; Léa El Khoury; David L Mobley
Journal:  J Comput Aided Mol Des       Date:  2019-11-28       Impact factor: 3.686

Review 3.  The structural evolution of β-secretase inhibitors: a focus on the development of small-molecule inhibitors.

Authors:  Stefania Butini; Simone Brogi; Ettore Novellino; Giuseppe Campiani; Arun K Ghosh; Margherita Brindisi; Sandra Gemma
Journal:  Curr Top Med Chem       Date:  2013       Impact factor: 3.295

Review 4.  BACE1 (β-secretase) inhibitors for the treatment of Alzheimer's disease.

Authors:  Arun K Ghosh; Heather L Osswald
Journal:  Chem Soc Rev       Date:  2014-10-07       Impact factor: 54.564

5.  Fragment-based Binding Efficiency Indices in Bioactive Molecular Design: A Computational Approach to BACE-1 Inhibitors.

Authors:  Nima Razzaghi-Asl; Ahmad Ebadi; Najmeh Edraki; Sara Shahabipour; Ramin Miri
Journal:  Iran J Pharm Res       Date:  2013       Impact factor: 1.696

6.  Exploring the binding of BACE-1 inhibitors using comparative binding energy analysis (COMBINE).

Authors:  Shu Liu; Rao Fu; Xiao Cheng; Sheng-Ping Chen; Li-Hua Zhou
Journal:  BMC Struct Biol       Date:  2012-08-27

Review 7.  New directions for protease inhibitors directed drug discovery.

Authors:  Yoshio Hamada; Yoshiaki Kiso
Journal:  Biopolymers       Date:  2016-11-04       Impact factor: 2.505

  7 in total

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