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Discovery and structure-activity relationship analysis of Staphylococcus aureus sortase A inhibitors.


ABSTRACT: Methicillin resistant Staphylococcus aureus (MRSA) is a major health problem that has created a pressing need for new antibiotics. Compounds that inhibit the S. aureus SrtA sortase may function as potent anti-infective agents as this enzyme attaches virulence factors to the cell wall. Using high-throughput screening, we have identified several compounds that inhibit the enzymatic activity of the SrtA. A structure-activity relationship (SAR) analysis led to the identification of several pyridazinone and pyrazolethione analogs that inhibit SrtA with IC(50) values in the sub-micromolar range. Many of these molecules also inhibit the sortase enzyme from Bacillus anthracis suggesting that they may be generalized sortase inhibitors.

SUBMITTER: Suree N 

PROVIDER: S-EPMC2888031 | biostudies-literature | 2009 Oct

REPOSITORIES: biostudies-literature

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Discovery and structure-activity relationship analysis of Staphylococcus aureus sortase A inhibitors.

Suree Nuttee N   Yi Sung Wook SW   Thieu William W   Marohn Melanie M   Damoiseaux Robert R   Chan Albert A   Jung Michael E ME   Clubb Robert T RT  

Bioorganic & medicinal chemistry 20090906 20


Methicillin resistant Staphylococcus aureus (MRSA) is a major health problem that has created a pressing need for new antibiotics. Compounds that inhibit the S. aureus SrtA sortase may function as potent anti-infective agents as this enzyme attaches virulence factors to the cell wall. Using high-throughput screening, we have identified several compounds that inhibit the enzymatic activity of the SrtA. A structure-activity relationship (SAR) analysis led to the identification of several pyridazin  ...[more]

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