Literature DB >> 23570791

Design and synthesis of thiophene dihydroisoquinolines as novel BACE1 inhibitors.

Ying-Zi Xu1, Shendong Yuan, Simeon Bowers, Roy K Hom, Wayman Chan, Hing L Sham, Yong L Zhu, Paul Beroza, Hu Pan, Eric Brecht, Nanhua Yao, Julie Lougheed, Jiangli Yan, Danny Tam, Zhao Ren, Lany Ruslim, Michael P Bova, Dean R Artis.   

Abstract

Utilizing a structure based design approach, combined with extensive medicinal chemistry execution, highly selective, potent and novel BACE1 inhibitor 8 (BACE1 Alpha assay IC50=8nM) was made from a weak μM potency hit in an extremely efficient way. The detailed SAR and general design approaches will be discussed.
Copyright © 2013 Elsevier Ltd. All rights reserved.

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Year:  2013        PMID: 23570791     DOI: 10.1016/j.bmcl.2013.03.009

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


  2 in total

1.  Fragment Binding to β-Secretase 1 without Catalytic Aspartate Interactions Identified via Orthogonal Screening Approaches.

Authors:  Frederik J R Rombouts; Richard Alexander; Erna Cleiren; Alex De Groot; Michel Carpentier; Joyce Dijkmans; Katleen Fierens; Stefan Masure; Diederik Moechars; Martina Palomino-Schätzlein; Antonio Pineda-Lucena; Andrés A Trabanco; Daan Van Glabbeek; Ann Vos; Gary Tresadern
Journal:  ACS Omega       Date:  2017-02-24

Review 2.  Development and Structural Modification of BACE1 Inhibitors.

Authors:  Ting Gu; Wen-Yu Wu; Ze-Xi Dong; Shao-Peng Yu; Ying Sun; Yue Zhong; Yu-Ting Lu; Nian-Guang Li
Journal:  Molecules       Date:  2016-12-22       Impact factor: 4.411

  2 in total

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