N-{3-[(1,1-dioxido-1,2-benzothiazol-3-yl)(phenyl)amino]propyl}benzamide analogs as potent Kv1.3 inhibitors. Part 1,Bioorganic & Medicinal Chemistry Letters

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N-{3-[(1,1-dioxido-1,2-benzothiazol-3-yl)(phenyl)amino]propyl}benzamide analogs as potent Kv1.3 inhibitors. Part 1
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2010-10-07 , DOI: 10.1016/j.bmcl.2010.09.132
Curt D. Haffner , Stephen A. Thomson , Yu Guo , Lee T. Schaller , Sharon Boggs , Scott Dickerson , Jeff Gobel , Dan Gillie , J. Patrick Condreay

We report the synthesis and in vitro activity of a series of novel N-{3-[(1,1-dioxido-1,2-benzothiazol-3-yl)(phenyl)amino]propyl}benzamide analogs. These analogs showed potent inhibitory activity against Kv1.3. Several compounds, including compound 8b, showed similar potency to the known Kv1.3 inhibitor PAP-1 when tested under the IonWorks patch clamp assay conditions.

中文翻译：

N- {3-[（1,1-二氧化物-1,2-苯并噻唑-3-基）（苯基）氨基]丙基}苯甲酰胺类似物作为有效的Kv1.3抑制剂。第1部分

我们报告了一系列新型N- {3-[（1,1-dioxido-1,2-苯并噻唑-3-基）（苯基）氨基]丙基}苯甲酰胺类似物的合成和体外活性。这些类似物显示出对Kv1.3的有效抑制活性。在IonWorks膜片钳测定条件下进行测试时，包括化合物8b在内的几种化合物显示出与已知Kv1.3抑制剂PAP-1相似的效力。

更新日期：2010-10-07

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