1417860-71-9Relevant academic research and scientific papers
Inhibitors of bacterial type III secretion system
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Page/Page column 27; 28, (2016/06/14)
Organic compounds showing the ability to inhibit effector toxin secretion or translocation mediated by bacterial type III secretion systems are disclosed. The disclosed type III secretion system inhibitor compounds are useful for combating infections by G
Synthesis and structure-activity relationships of novel phenoxyacetamide inhibitors of the Pseudomonas aeruginosa type III secretion system (T3SS)
Williams, John D.,Torhan, Matthew C.,Neelagiri, Venugopal R.,Brown, Carson,Bowlin, Nicholas O.,Di, Ming,McCarthy, Courtney T.,Aiello, Daniel,Peet, Norton P.,Bowlin, Terry L.,Moir, Donald T.
, p. 1027 - 1043 (2015/03/04)
The increasing prevalence of drug-resistant bacterial infections is driving the discovery and development not only of new antibiotics, but also of inhibitors of virulence factors that are crucial for in vivo pathogenicity. One such virulence factor is the type III secretion system (T3SS), which plays a critical role in the establishment and dissemination of Pseudomonas aeruginosa infections. We have recently described the discovery and characterization of a series of inhibitors of P. aeruginosa T3SS based on a phenoxyacetamide scaffold. To better characterize the factors involved in potent T3SS inhibition, we have conducted a systematic exploration of this structure, revealing several highly responsive structure-activity relationships indicative of interaction with a specific target. Most of the structural features contributing to potency were additive, and combination of those features produced optimized inhibitors with IC50 values 1 μM.
