Design and synthesis of brain penetrant selective JNK inhibitors with improved pharmacokinetic properties for the prevention of neurodegeneration
Design and synthesis of brain penetrant selective JNK inhibitors with improved pharmacokinetic properties for the prevention of neurodegeneration
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DOI：
10.1016/j.bmcl.2011.06.100
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发表时间：
2011-09-15
影响因子：
2.7
通讯作者：
Griswold-Prenner, Irene
中科院分区：
文献类型：
--
作者：
Bowers, Simeon;Truong, Anh P.;Griswold-Prenner, Irene
描述了一系列具有改善的药代动力学性质的脑渗透剂、基于三取代噻吩的JNK抑制剂的SAR。这些化合物是基于代谢物鉴定研究的信息设计的，与早期类似物相比，代谢物鉴定研究导致化合物如42具有较低的清除率、更大的脑暴露和更长的半衰期。(C)2011爱思唯尔有限公司保留所有权利。
The SAR of a series of brain penetrant, trisubstituted thiophene based JNK inhibitors with improved pharmacokinetic properties is described. These compounds were designed based on information derived from metabolite identification studies which led to compounds such as 42 with lower clearance, greater brain exposure and longer half life compared to earlier analogs. (C) 2011 Elsevier Ltd. All rights reserved.