Novel inhibitors of neuronal nitric oxide synthase with potent antioxidant properties
Novel inhibitors of neuronal nitric oxide synthase with potent antioxidant properties
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DOI：
10.1016/s0960-894x(02)00883-1
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发表时间：
2003-01-20
影响因子：
2.7
通讯作者：
Chabrier, PE
中科院分区：
文献类型：
--
作者：
Auvin, S;Auguet, M;Chabrier, PE
合成了一系列具有nNOS药效团与抗氧化剂片段相连的杂化化合物。其中，化合物8d是一种异丙酚衍生物，具有最强的抗nNOS(IC50=0.12um)和脂质过氧化(IC50=0.4um)的双重效力，并具有e/nNOS选择性(67.5)。这表明nNOS能够在其活性中心容纳非常大的基团，如二叔丁基或二异丙基苯酚。(C)2002爱思唯尔科学有限公司。保留所有权利。
A series of hybrid compounds possessing an nNOS pharmacophore linked to an antioxidant fragment has been synthesized. Among them, compound 8d, a propofol derivative, displayed the greatest dual potencies against nNOS (IC50 = 0.12 muM) and lipid peroxidation (IC50 = 0.4 muM) accompanied with e/nNOS selectivity (67.5). This shows that nNOS was able to accommodate very bulky groups such as di-tert-butyl or di-iso-propyl phenol in its active site. (C) 2002 Elsevier Science Ltd. All rights reserved.