Bridged tetrahydroisoquinolines as selective NADPH oxidase 2 (Nox2) inhibitors.
Bridged tetrahydroisoquinolines as selective NADPH oxidase 2 (Nox2) inhibitors.
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DOI：
10.1039/c3md00061c
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发表时间：
2013-07
期刊：
影响因子：
--
通讯作者：
Skoda EM
中科院分区：
文献类型：
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作者：
Cifuentes-Pagano E;Saha J;Csányi G;Ghouleh IA;Sahoo S;Rodríguez A;Wipf P;Pagano PJ;Skoda EM
(1SR 4 RS）-3，3-二甲基-1，2，3，4-四氢-1，4-（差向亚氨基甲烷）萘由市售材料经2-3步合成，并评估其在一系列Nox亚型中的特异性和有效性。N-戊基和N-亚甲基噻吩取代的类似物11 g和11 h显示为选择性Nox 2抑制剂，细胞IC 50值分别为20和32 μM。
(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 μM, respectively.