Dyes of formula (1), their production and their use.
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(2016/04/20)
A reverse method for diversity introduction of benzimidazole to synthesize H+/K+-ATP enzyme inhibitors
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 14l (IC50 = 1.6 × 10-5 M) was comparable with H+/K+-ATP enzyme inhibitor in vitro.
Yan, Yu,Liu, Zijie,Zhang, Jianjun,Xu, Ruiming,Hu, Xiao,Liu, Gang