Discovery of non-carbohydrate inhibitors of aminoglycoside-modifying enzymes

…, NA Whittemore, C Özen, E Wright, CL Brown…

Index: Welch, Karen T.; Virga, Kristopher G.; Whittemore, Neil A.; Oezen, Can; Wright, Edward; Brown, Cynthia L.; Lee, Richard E.; Serpersu, Engin H. Bioorganic and Medicinal Chemistry, 2005 , vol. 13, # 22 p. 6252 - 6263

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Citation Number: 34

Abstract

Chemical modification and inactivation of aminoglycosides by many different enzymes expressed in pathogenic bacteria are the main mechanisms of bacterial resistance to these antibiotics. In this work, we designed inhibitors that contain the 1, 3-diamine pharmacophore shared by all aminoglycoside antibiotics that contain the 2-deoxystreptamine ring. A discovery library of molecules was prepared by attaching different side chains to both ...