期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 23, 期 20, 页码 5503-5506出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2013.08.070
关键词
Natural products; Ion channel inhibitors; Indoles; Thiolation; Electrophysiology
资金
- Natural Science and Engineering Research (NSERC) of Canada
- University of Alberta
The first synthesis of the non-peptidic snail toxin 6-bromo-2-mercaptotryptamine dimer (BrMT)(2) is described, along with the preparation of its lower and higher thio homologs. The synthetic (BrMT)(2) and its derivatives reported herein are all capable of slowing the activation of the K(v)1.1 potassium ion channel. Only the monosulfide variant shows significant slowing of the deactivation process. This synthetic strategy can now be applied to creating a more extensive set of compounds that vary in the length of the linker connecting the two monomers, the substituents on the indole ring core, and terminal amine. (C) 2013 Elsevier Ltd. All rights reserved.
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