Literature DB >> 18842420

Design, synthesis and SAR of potent statine-based BACE-1 inhibitors: exploration of P1 phenoxy and benzyloxy residues.

Marcus Bäck1, Jonas Nyhlén, Ingemar Kvarnström, Sara Appelgren, Neera Borkakoti, Katarina Jansson, Jimmy Lindberg, Susanne Nyström, Anders Hallberg, Sa Rosenquist, Bertil Samuelsson.   

Abstract

Several BACE-1 inhibitors with low nanomolar level activities, encompassing a statine-based core structure with phenyloxymethyl- and benzyloxymethyl residues in the P1 position, are presented. The novel P1 modification introduced to allow the facile exploration of the S1 binding pocket of BACE-1, delivered highly promising inhibitors.

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Year:  2008        PMID： 18842420     DOI： 10.1016/j.bmc.2008.09.041

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN： 0968-0896            Impact factor:   3.641


  6 in total

1.  Asymmetric synthesis of anti-aldol segments via a nonaldol route: synthetic applications to statines and (-)-tetrahydrolipstatin.

Authors:  Arun K Ghosh; Khriesto Shurrush; Sarang Kulkarni
Journal:  J Org Chem       Date:  2009-06-19       Impact factor: 4.354

Review 2.  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

3.  Design and Synthesis of Novel Arylketo-containing P1-P3 Linked Macro-cyclic BACE-1 Inhibitors.

Authors:  Veronica Sandgren; Oscar Belda; Ingemar Kvarnström; Jimmy Lindberg; Bertil Samuelsson; Anders Dahlgren
Journal:  Open Med Chem J       Date:  2015-03-31

4.  Design and Synthesis of Hydroxyethylene-Based BACE-1 Inhibitors Incorporating Extended P1 Substituents.

Authors:  Veronica Sandgren; Marcus Bäck; Ingemar Kvarnström; Anders Dahlgren
Journal:  Open Med Chem J       Date:  2013-03-08

5.  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

6.  Virtual screening and structure-based discovery of indole acylguanidines as potent β-secretase (BACE1) inhibitors.

Authors:  Yiquan Zou; Li Li; Wuyan Chen; Tiantian Chen; Lanping Ma; Xin Wang; Bing Xiong; Yechun Xu; Jingkang Shen
Journal:  Molecules       Date:  2013-05-16       Impact factor: 4.411
  6 in total

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