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

ABSTRACT: Bacterial resistance to ?-lactam antibiotics caused by class B metallo-?-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.

SUBMITTER: Chen P

PROVIDER: S-EPMC3463135 | biostudies-literature | 2012 Oct

REPOSITORIES: biostudies-literature

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

Chen Pinhong P Horton Lori B LB Mikulski Rose L RL Deng Lisheng L Sundriyal Sandeep S Palzkill Timothy T Song Yongcheng Y

Bioorganic & medicinal chemistry letters 20120810 19

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. ...[more]

PMID: 22921080

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