SAR investigations on a novel class of gamma-secretase modulators based on a unique scaffold

被引：6

作者：

Austin, Wesley F. ^{[1
]}

Hubbs, Jed L. ^{[1
]}

Fuller, Nathan O. ^{[1
]}

Creaser, Steffen P. ^{[1
]}

McKee, Timothy D. ^{[1
]}

Loureiro, Robyn M. B. ^{[1
]}

Findeis, Mark A. ^{[1
]}

Tate, Barbara ^{[1
]}

Ives, Jeffrey L. ^{[1
]}

Bronk, Brian S. ^{[1
]}

机构：

[1] Satori Pharmaceut, Cambridge, MA 02139 USA

来源：

MEDCHEMCOMM | 2013年 / 4卷 / 03期

关键词：

ALZHEIMERS-DISEASE; OPTIMIZATION; HYPOTHESIS; INHIBITORS; A-BETA-40;

D O I：

10.1039/c3md20357c

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

In this communication we present details of our analog efforts within a novel series of gamma-secretase modulating compounds. Esters and carbamates were investigated as bioisosteres for a glycoside moiety present in an initial hit isolated from black cohosh extract. We identified elements within each series that retain the potency and selectivity of the initial lead while improving physicochemical properties.

引用

页码：569 / 574

页数：6

共 24 条

[1]

Alzheimer's Association, 2012, 2012 ALZH DIS FACTS

[2]

[Anonymous], 2010, NIH PUBL

[3] γ-secretase modulation and its promise for Alzheimer's disease:: A rationale for drug discovery [J].