Bioorganic and Medicinal Chemistry Letters p. 4189 - 4192 (2011)
Update date:2022-08-05
Topics:
Yan, Yu
Liu, Zijie
Zhang, Jianjun
Xu, Ruiming
Hu, Xiao
Liu, Gang
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.
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Doi:10.1002/ejoc.201100726
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