Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, 2 Nanwei Rd., Xicheng Dist., Beijing 100050, PR China.
Bioorg Med Chem Lett. 2011 Jul 15;21(14):4189-92. doi: 10.1016/j.bmcl.2011.05.080. Epub 2011 May 27.
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 (IC(50)=1.6×10(-5)M) was comparable with H(+)/K(+)-ATP enzyme inhibitor in vitro.
一系列 2-[(2-吡啶基甲基)亚磺酰基]苯并咪唑衍生物通过使用反相多样性引入方法的溶液相合成路线合成。使用这种合成策略，我们同时获得了两个关键中间体（4-A 和 4-B），这使得我们能够在可靠的反应条件下将多样性点引入最终产物的苯并咪唑部分，以鉴定有效的 H(+)/K(+)-ATP 酶抑制剂。化合物 14l（IC(50)=1.6×10(-5)M）与体外 H(+)/K(+)-ATP 酶抑制剂相当。
