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

…, W Thieu, M Marohn, R Damoiseaux, A Chan…

Index: Suree, Nuttee; Yi, Sung Wook; Thieu, William; Marohn, Melanie; Damoiseaux, Robert; Chan, Albert; Jung, Michael E.; Clubb, Robert T. Bioorganic and Medicinal Chemistry, 2009 , vol. 17, # 20 p. 7174 - 7185

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Citation Number: 66

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 ( ...