Design, synthesis, and in vivo activity of novel inhibitors of delta-5 desaturase for the treatment of metabolic syndrome
Design, synthesis, and in vivo activity of novel inhibitors of delta-5 desaturase for the treatment of metabolic syndrome
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DOI：
10.1016/j.bmcl.2015.07.066
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发表时间：
2015-09-15
影响因子：
2.7
通讯作者：
Lombardo, Victoria K.
中科院分区：
文献类型：
--
作者：
Baugh, Simon D. P.;Pabba, Praveen K.;Lombardo, Victoria K.
描述了δ -5去饱和酶抑制剂的合成、SAR和体内活性。初始系列的环约束提供了多种体外活性化型，从中选择了吲哚唑。从吲哚唑系列的例子显示出体内活性降低肝脏δ -5去饱和酶的酶活性。(C) 2015 Elsevier Ltd.版权所有。
The synthesis, SAR, and in vivo activity of inhibitors of delta-5 desaturase are described. Ring-constraint of the initial series provided access to a variety of in vitro active chemotypes, from which the indazole was selected. Examples from the indazole series displayed in vivo activity in reducing the enzymatic activity of liver delta-5 desaturase. (C) 2015 Elsevier Ltd. All rights reserved.