BACE1 inhibitors: A head group scan on a series of amides
详细信息 查看全文
- 作者：Thomas J. Woltering ; Wolfgang Wostl ; Hans Hilpert ; Mark Rogers-Evans ; Emmanuel Pinard ; Alex ; er Mayweg ; Martin G?bel ; David W. Banner ; J?rg Benz ; Massimiliano Travagli ; Martina Pollastrini ; Guido Marconi ; Emanuele Gabellieri ; Wolfgang Guba ; Harald Mauser ; Matteo Andreini ; Helmut Jacobsen ; Eoin Power ; Robert Narquizian
- 关键词：BACE1 ; Alzheimer&rsquo ; s disease ; Inhibitors ; pKa ; P-gp
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2013
- 出版时间：15 July, 2013
- 年：2013
- 卷：23
- 期：14
- 页码：4239-4243
- 全文大小：2159 K
文摘
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.