Bridged tetrahydroisoquinolines as selective NADPH oxidase 2 (Nox2) inhibitors

桥联四氢异喹啉类化合物作为选择性 NADPH 氧化酶 2 (Nox2) 抑制剂

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Abstract

(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 IC(50) values of 20 and 32 μM, respectively.

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