Bridged tetrahydroisoquinolines as selective NADPH oxidase 2 (Nox2) inhibitors

被引：26

作者：

Cifuentes-Pagano, Eugenia ^{[1
]}

Saha, Jaideep ^{[1
,2
]}

Csanyi, Gabor ^{[1
]}

Al Ghouleh, Imad ^{[1
]}

Sahoo, Sanghamitra ^{[1
]}

Rodriguez, Andres ^{[1
]}

Wipf, Peter ^{[2
,3
]}

Pagano, Patrick J. ^{[1
]}

Skoda, Erin M. ^{[2
]}

机构：

[1] Univ Pittsburgh, Dept Pharmacol & Chem Biol, Vasc Med Inst, Pittsburgh, PA 15260 USA

[2] Univ Pittsburgh, Dept Chem, Ctr Chem Methodol & Lib Dev, Pittsburgh, PA 15261 USA

[3] Univ Pittsburgh, Dept Pharmaceut Sci, Pittsburgh, PA 15260 USA

来源：

MEDCHEMCOMM | 2013年 / 4卷 / 07期

基金：

美国国家卫生研究院;

关键词：

OXIDATIVE STRESS; SUPEROXIDE; ACTIVATION; DISEASE; FAMILY; ROS; DERIVATIVES; EXPRESSION; PROTEINS; ZINC;

D O I：

10.1039/c3md00061c

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：

(1SR,4RS)-3,3-Dimethyl-1,2,3,4-tetrahydro-1,4-(epiminomethano)naphthalenes were synthesized in 2-3 steps from commercially available materials and assessed for specificity and effectiveness across a range of Nox isoforms. The N-pentyl and N-methylenethiophene substituted analogs 11g and 11h emerged as selective Nox2 inhibitors with cellular IC50 values of 20 and 32 mu M, respectively.

引用

页码：1085 / 1092

页数：8

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