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A reverse method for diversity introduction of benzimidazole to synthesize H(+)/K(+)-ATP enzyme inhibitors

Authors:	Yan Yu Liu Zijie Zhang Jianjun Xu Ruiming Hu Xiao Liu Gang

Institution:	^a Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, 2 Nanwei Rd., Xicheng Dist., Beijing 100050, PR China ^b Department of Pharmacology and Pharmaceutical Sciences, School of Medicine, Tsinghua University, Haidian Dist., Beijing 100084, PR China

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 14l (IC₅₀ = 1.6 × 10⁻⁵ M) was comparable with H⁺/K⁺-ATP enzyme inhibitor in vitro.

Keywords:	Benzimidazole H⁺/K⁺-ATP enzyme inhibitors DFDNB Solution phase synthesis
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