Synthesis and BK channel-opening activity of 2-amino-1,3-thiazole derivatives

被引：4
作者：
Qi, Xiao-Lei [1 ]
Jo, Heeji [2 ,3 ]
Wang, Xue-Ying [1 ]
Ji, Tong-Tong [1 ]
Lin, Hai-Xia [1 ]
Park, Chul-Seung [2 ,3 ]
Cui, Yong-Mei [1 ]
机构：
[1] Shanghai Univ, Coll Sci, Innovat Drug Res Ctr, Dept Chem, Shanghai 200444, Peoples R China
[2] Gwangju Inst Sci & Technol GIST, Sch Life Sci, Gwangju 61005, South Korea
[3] Gwangju Inst Sci & Technol GIST, Natl Leading Res Lab, Gwangju 61005, South Korea
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2021年 / 43卷
关键词：
BK channels; Openers; Synthesis; Thiazole; SAR; ACTIVATED POTASSIUM CHANNELS; SMOOTH-MUSCLE; K+ CHANNELS; PHARMACOLOGICAL ACTIVATION; TRANSMITTER RELEASE; SKELETAL-MUSCLE; BETA-SUBUNIT; BLADDER; CONTRACTILITY; EXCITABILITY;
D O I：
10.1016/j.bmcl.2021.128083
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of 2-amino-5-arylmethyl-or 5-heteroarylmethyl-1,3-thiazole derivatives were synthesized and evaluated for BK channel-opening activities in cell-based fluorescence assay and electrophysiological recording. The assay results indicated that the activities of the investigated compounds were influenced by the physicochemical properties of the substituent at benzene ring.
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页数：6
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