2-Substituted 4, 5-dihydrothiazole-4-carboxylic acids are novel inhibitors of metallo-β-lactamases

…, LB Horton, RL Mikulski, L Deng, S Sundriyal…

Index: Chen, Pinhong; Horton, Lori B.; Mikulski, Rose L.; Deng, Lisheng; Sundriyal, Sandeep; Palzkill, Timothy; Song, Yongcheng Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 19 p. 6229 - 6232

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Citation Number: 21

Abstract

Bacterial resistance to β-lactam antibiotics caused by class B metallo-β-lactamases (MBL), especially for certain hospital-acquired, Gram-negative pathogens, poses a significant threat to public health. We report several 2-substituted 4, 5-dihydrothiazole-4-carboxylic acids to be novel MBL inhibitors. Structure activity relationship (SAR) and molecular modeling studies were performed and implications for further inhibitor design are discussed.