Discovery of biaryl inhibitors of H+/K+ ATPase

…, I Farre-Gutierrez, G Hutley, G Bravi, P Pickering

文献索引：Garton, Neil; Bailey, Nick; Bamford, Mark; Demont, Emmanuel; Farre-Gutierrez, Irene; Hutley, Gail; Bravi, Gianpaolo; Pickering, Paula Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 3 p. 1049 - 1054

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被引用次数: 9

摘要

We report the identification of a novel biaryl template for H+/K+ ATPase inhibition. Evaluation of critical SAR features within the biaryl imidazole framework and the use of pharmacophore modelling against known imidazopyridine and azaindole templates suggested that the geometry of the molecule is key to achieving activity. Herein we present our work optimising the potency of the molecule through modifications and substitutions to ...