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.

journal_name

Bioorg Med Chem

authors

Suree N,Yi SW,Thieu W,Marohn M,Damoiseaux R,Chan A,Jung ME,Clubb RT

doi

10.1016/j.bmc.2009.08.067

subject

Has Abstract

pub_date

2009-10-15 00:00:00

pages

7174-85

issue

20

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(09)00841-4

journal_volume

17

pub_type

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