SAR of α7 nicotinic receptor agonists derived from tilorone: Exploration of a novel nicotinic pharmacophore
SAR of α7 nicotinic receptor agonists derived from tilorone: Exploration of a novel nicotinic pharmacophore
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DOI：
10.1016/j.bmcl.2011.12.126
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发表时间：
2012-02-15
影响因子：
2.7
通讯作者：
Meyer, Michael D.
中科院分区：
文献类型：
--
作者：
Schrimpf, Michael R.;Sippy, Kevin B.;Meyer, Michael D.
众所周知的干扰素诱导剂替洛龙被发现对α 7神经元烟碱受体的激动剂位点具有有效的亲和力（Ki = 56 nM）。SAR调查确定，这两个基本的侧链是必不可少的有效的活动，但活性单取代的衍生物也可以制备，如果灵活的侧链取代构象刚性的环胺。类似物，其中的芴酮核心被取代的二苯并噻吩-5，5-二氧化物或吨酮也保留有效的活性。(C)2012爱思唯尔有限公司保留所有权利。
The well-known interferon-inducer tilorone was found to possess potent affinity for the agonist site of the alpha 7 neuronal nicotinic receptor (K-i = 56 nM). SAR investigations determined that both basic sidechains are essential for potent activity, however active monosubstituted derivatives can also be prepared if the flexible sidechains are replaced with conformationally rigidified cyclic amines. Analogs in which the fluorenone core is replaced with either dibenzothiophene-5,5-dioxide or xanthenone also retain potent activity. (C) 2012 Elsevier Ltd. All rights reserved.