Literature DB >> 23735744

BACE1 inhibitors: a head group scan on a series of amides.

Thomas J Woltering1, Wolfgang Wostl, Hans Hilpert, Mark Rogers-Evans, Emmanuel Pinard, Alexander Mayweg, Martin Göbel, David W Banner, Jörg Benz, Massimiliano Travagli, Martina Pollastrini, Guido Marconi, Emanuele Gabellieri, Wolfgang Guba, Harald Mauser, Matteo Andreini, Helmut Jacobsen, Eoin Power, Robert Narquizian.   

Abstract

A series of amides bearing a variety of amidine head groups was investigated as BACE1 inhibitors with respect to inhibitory activity in a BACE1 enzyme as well as a cell-based assay. Determination of their basicity as well as their properties as substrates of P-glycoprotein revealed that a 2-amino-1,3-oxazine head group would be a suitable starting point for further development of brain penetrating compounds for potential Alzheimer's disease treatment.
Copyright © 2013 Elsevier Ltd. All rights reserved.

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Year:  2013        PMID： 23735744     DOI： 10.1016/j.bmcl.2013.05.003

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


  10 in total

Review 1.  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

2.  Development of 2-aminooxazoline 3-azaxanthene β-amyloid cleaving enzyme (BACE) inhibitors with improved selectivity against Cathepsin D.

Authors:  Jonathan D Low; Michael D Bartberger; Kui Chen; Yuan Cheng; Mark R Fielden; Vijay Gore; Dean Hickman; Qingyian Liu; E Allen Sickmier; Hugo M Vargas; Jonathan Werner; Ryan D White; Douglas A Whittington; Stephen Wood; Ana E Minatti
Journal:  Medchemcomm       Date:  2017-04-27       Impact factor: 3.597

3.  Aminomethyl-Derived Beta Secretase (BACE1) Inhibitors: Engaging Gly230 without an Anilide Functionality.

Authors:  Christopher R Butler; Kevin Ogilvie; Luis Martinez-Alsina; Gabriela Barreiro; Elizabeth M Beck; Charles E Nolan; Kevin Atchison; Eric Benvenuti; Leanne Buzon; Shawn Doran; Cathleen Gonzales; Christopher J Helal; Xinjun Hou; Mei-Hui Hsu; Eric F Johnson; Kimberly Lapham; Lorraine Lanyon; Kevin Parris; Brian T O'Neill; David Riddell; Ashley Robshaw; Felix Vajdos; Michael A Brodney
Journal:  J Med Chem       Date:  2016-12-20       Impact factor: 7.446

Review 4.  Highlights in BACE1 Inhibitors for Alzheimer's Disease Treatment.

Authors:  Judite R M Coimbra; Daniela F F Marques; Salete J Baptista; Cláudia M F Pereira; Paula I Moreira; Teresa C P Dinis; Armanda E Santos; Jorge A R Salvador
Journal:  Front Chem       Date:  2018-05-24       Impact factor: 5.221

5.  Synthesis and Transformation of (-)-Isopulegol-Based Chiral β-Aminolactones and β-Aminoamides.

Authors:  Tam Minh Le; Péter Bérdi; István Zupkó; Ferenc Fülöp; Zsolt Szakonyi
Journal:  Int J Mol Sci       Date:  2018-11-08       Impact factor: 5.923

6.  Au-catalyzed skeletal rearrangement of O-propargylic oximes via N-O bond cleavage with the aid of a Brønsted base cocatalyst.

Authors:  Keigo Shiga; Ilya D Gridnev; Masahiro Terada; Itaru Nakamura
Journal:  Chem Sci       Date:  2019-04-18       Impact factor: 9.825

Review 7.  Fluorinated Molecules and Nanotechnology: Future 'Avengers' against the Alzheimer's Disease?

Authors:  Meghna Dabur; Joana A Loureiro; Maria Carmo Pereira
Journal:  Int J Mol Sci       Date:  2020-04-23       Impact factor: 5.923

8.  Mapping the conformational space accessible to catechol-O-methyltransferase.

Authors:  Andreas Ehler; Jörg Benz; Daniel Schlatter; Markus G Rudolph
Journal:  Acta Crystallogr D Biol Crystallogr       Date:  2014-07-25

9.  Design of Curcumin and Flavonoid Derivatives with Acetylcholinesterase and Beta-Secretase Inhibitory Activities Using in Silico Approaches.

Authors:  Thai-Son Tran; Minh-Tri Le; Thanh-Dao Tran; The-Huan Tran; Khac-Minh Thai
Journal:  Molecules       Date:  2020-08-10       Impact factor: 4.411

10.  Synthesis, In Silico and In Vitro Evaluation for Acetylcholinesterase and BACE-1 Inhibitory Activity of Some N-Substituted-4-Phenothiazine-Chalcones.

Authors:  Thai-Son Tran; Minh-Tri Le; Thi-Cam-Vi Nguyen; The-Huan Tran; Thanh-Dao Tran; Khac-Minh Thai
Journal:  Molecules       Date:  2020-08-27       Impact factor: 4.411
  10 in total

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