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.

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 (IC501.6 x 10-5M) was comparable with H+/K+-ATP enzyme inhibitor in vitro.......