Literature DB >> 16263281

Conformationally biased P3 amide replacements of beta-secretase inhibitors.

Shawn J Stachel1, Craig A Coburn, Thomas G Steele, Min-Chi Crouthamel, Beth L Pietrak, Ming-Tain Lai, M Katharine Holloway, Sanjeev K Munshi, Samuel L Graham, Joseph P Vacca.   

Abstract

We have synthesized and evaluated a series of conformationally biased P3 amide replacements based on an isophthalamide lead structure. The studies resulted in the identification of the beta-secretase inhibitor 7m which has an in vitro IC(50)=35 nM. The synthesis and biological activities of these compounds are described.

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Year:  2005        PMID： 16263281     DOI： 10.1016/j.bmcl.2005.10.032

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


  14 in total

1.  Developing consensus 3D-QSAR and pharmacophore models for several beta-secretase, farnesyl transferase and histone deacetylase inhibitors.

Authors:  Hsin-Yuan Wei; Guan-Ju Chen; Chih-Lun Chen; Thy-Hou Lin
Journal:  J Mol Model       Date:  2011-05-12       Impact factor: 1.810

2.  pH-dependent conformational dynamics of beta-secretase 1: A molecular dynamics study.

Authors:  Daniel J Mermelstein; J Andrew McCammon; Ross C Walker
Journal:  J Mol Recognit       Date:  2018-09-27       Impact factor: 2.137

3.  Molecular shape and medicinal chemistry: a perspective.

Authors:  Anthony Nicholls; Georgia B McGaughey; Robert P Sheridan; Andrew C Good; Gregory Warren; Magali Mathieu; Steven W Muchmore; Scott P Brown; J Andrew Grant; James A Haigh; Neysa Nevins; Ajay N Jain; Brian Kelley
Journal:  J Med Chem       Date:  2010-05-27       Impact factor: 7.446

4.  Phenotypic assays for β-amyloid in mouse embryonic stem cell-derived neurons.

Authors:  Laura Beth J McIntire; Natalie Landman; Min Suk Kang; Gina M Finan; Jeremy C Hwang; Ann Z Moore; Lydia S Park; Chyuan-Sheng Lin; Tae-Wan Kim
Journal:  Chem Biol       Date:  2013-07-25

5.  Molecular modeling, synthesis, and activity studies of novel biaryl and fused-ring BACE1 inhibitors.

Authors:  Srinivas Reddy Chirapu; Boobalan Pachaiyappan; Hikmet F Nural; Xin Cheng; Hongbin Yuan; David C Lankin; Samer O Abdul-Hay; Gregory R J Thatcher; Yong Shen; Alan P Kozikowski; Pavel A Petukhov
Journal:  Bioorg Med Chem Lett       Date:  2008-10-25       Impact factor: 2.823

6.  Retrospective molecular docking study of WY-25105 ligand to β-secretase and bias of the three-dimensional structure flexibility.

Authors:  Leo Ghemtio; Nicolas Muzet
Journal:  J Mol Model       Date:  2013-04-07       Impact factor: 1.810

7.  Comparative molecular field analysis and comparative molecular similarity indices analysis of hydroxyethylamine derivatives as selective human BACE-1 inhibitor.

Authors:  Ashish Pandey; Jignesh Mungalpara; C Gopi Mohan
Journal:  Mol Divers       Date:  2009-03-28       Impact factor: 2.943

Review 8.  The "Sticky Patch" Model of Crystallization and Modification of Proteins for Enhanced Crystallizability.

Authors:  Zygmunt S Derewenda; Adam Godzik
Journal:  Methods Mol Biol       Date:  2017

Review 9.  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

10.  Sulfur-containing therapeutics in the treatment of Alzheimer's disease.

Authors:  Haizhou Zhu; Venkateshwara Dronamraju; Wei Xie; Swati S More
Journal:  Med Chem Res       Date:  2021-01-15       Impact factor: 1.965
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