Literature DB >> 18434152

Synthesis, SAR, and X-ray structure of human BACE-1 inhibitors with cyclic urea derivatives.

Heuisul Park1, Kyeongsik Min, Hyo-Shin Kwak, Ki Dong Koo, Dongchul Lim, Sang-Won Seo, Jae-Ung Choi, Bettina Platt, Deog-Young Choi.   

Abstract

We describe synthesis and evaluation of a series of cyclic urea derivatives with hydroxylethylamine isostere. Modification of P3, P1, and P2' and combination of SAR display a >100-fold increase in potency with good cellular activity (IC(50)=0.15microM) relative to the previously reported compound 3.

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Year:  2008        PMID: 18434152     DOI: 10.1016/j.bmcl.2008.03.081

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


  3 in total

1.  In silico screening of potential β-secretase (BACE1) inhibitors from VIETHERB database.

Authors:  Nguyen Thao Nhung; Nhung Duong; Huong Thi Thu Phung; Quan V Vo; Nguyen Minh Tam
Journal:  J Mol Model       Date:  2022-02-14       Impact factor: 1.810

2.  Cu(I)-catalyzed diamination of disubstituted terminal olefins: an approach to potent NK1 antagonist.

Authors:  Yuehong Wen; Baoguo Zhao; Yian Shi
Journal:  Org Lett       Date:  2009-06-04       Impact factor: 6.005

3.  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

  3 in total

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