Optimization of halopemide for phospholipase D2 inhibition
Optimization of halopemide for phospholipase D2 inhibition
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DOI：
10.1016/j.bmcl.2007.01.059
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发表时间：
2007-04-15
影响因子：
2.7
通讯作者：
Steed, Paul
中科院分区：
文献类型：
--
作者：
Monovich, Lauren;Mugrage, Benjamin;Steed, Paul
HTS 鉴定出卤哌胺可抑制磷脂酶 D2 (PLD2)，这为探索性地鉴定用作炎症介质的 PLD2 强抑制剂提供了基础。利用并行合成和纯化来快速鉴定源自吲哚 2-羧酸的口服酰胺类似物，其效力优于 PLD2。 (c) 2007 Elsevier Ltd. 保留所有权利。
Halopemide, which was identified by HTS to inhibit phospholipase D2 (PLD2), provided the basis for an exploratory effort to identify potent inhibitors of PLD2 for use as inflammatory mediators. Parallel synthesis and purification were utilized to rapidly identify orally available amide analogs derived from indole 2-carboxylic acids with superior potency versus PLD2. (c) 2007 Elsevier Ltd. All rights reserved.