5509-73-9Relevant 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.
The Reaction of 2-Substituted-4,5-dichloro-3(2H)-pyridazinones with Alkoxides and Alkylthiolates
Lyga, John W.
, p. 1757 - 1760 (2007/10/02)
The reaction of 2-substituted-4,5-dichloro-3(2H)-pyridazinones 1a-b with alkoxides and alkylthiolates was investigated.Regiospecific displacement of either the 4 or 5 chlorine atom could be achieved in most cases by appropriate selection of the reaction solvent.
