1035451-05-8Relevant academic research and scientific papers
Discovery and structure-activity relationship analysis of Staphylococcus aureus sortase A inhibitors
Suree, Nuttee,Yi, Sung Wook,Thieu, William,Marohn, Melanie,Damoiseaux, Robert,Chan, Albert,Jung, Michael E.,Clubb, Robert T.
experimental part, p. 7174 - 7185 (2010/03/30)
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 IC50 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.
PYRIDAZINONES AND FURAN-CONTAINING COMPOUNDS
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Page/Page column 97, (2008/12/07)
The present invention is directed to pyridazinone compounds of formula (I) and furan compounds of formula (II), pharmaceutical compositions of compounds of formula (I) and (II), kits containing these compounds, methods of syntheses, and a method of treatment of a proliferative disease in a subject by administration of a therapeutically effective amount of a compound of formulae (I) or (II). Both classes of compounds were identified through screening of a collection of small molecule libraries.
