ω-芋螺毒素GVIA的低分子量非肽模拟物。
Low molecular weight non-peptide mimics of omega-conotoxin GVIA.
作者信息
Duggan Peter J, Lewis Richard J, Phei Lok Y, Lumsden Natalie G, Tuck Kellie L, Yang Aijun
机构信息
CSIRO Molecular and Health Technologies, Clayton, VIC, Australia.
出版信息
Bioorg Med Chem Lett. 2009 May 15;19(10):2763-5. doi: 10.1016/j.bmcl.2009.03.130. Epub 2009 Mar 28.
We report the synthesis and biological activity of a low molecular weight non-peptidic mimic of the analgesic peptide omega-conotoxin GVIA. The molecular weight of this compound presents a reduction by 193g/mol compared to a previously reported lead. This compound exhibits an EC(50) of 5.8microM and is accessible in only six synthetic steps compared to the original lead (13 steps). We also report several improvements to the original synthetic route.
我们报告了一种低分子量非肽类镇痛肽ω-芋螺毒素GVIA模拟物的合成及其生物活性。与先前报道的先导化合物相比，该化合物的分子量降低了193g/mol。该化合物的半数有效浓度（EC50）为5.8μM，与原始先导化合物（13步）相比，仅需6步合成即可获得。我们还报告了对原始合成路线的若干改进。
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