学术论文
Yu YAN, Jianjun ZHANG, Zijie LIU, Ruiming XU, Xiao HU, Gang LIU*, A reversal method of diversity introduction of benzimidazole to synthesize H+/K+-ATP enzyme inhibitors. Bioorg Med Chem Lett. 2011 Jul 15;21(14):4189-92. Epub 2011 May 27.
发布时间:2011-11-16作者:刘刚关键字:
Abstract
A series of 2-[(2-pyridylmethyl)sulfinyl]benzimidazole derivatives were synthesized via a solution phase synthetic route using a reversal method of diversity introduction. Using this synthetic strategy, we obtained two key intermediates (4-A and 4-B) simultaneously, which allows us to introduce diversity points onto the benzimidazole part of the final product under reliable reaction conditions to identify potent H+/K+-ATP enzyme inhibitors. Compound 141 (IC50 1.6 x 10-5 M) was comparable with H+/K+-ATP enzyme inhibitor in vitro.
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