Synthesis and structure-activity relationships of novel phenoxyacetamide inhibitors of the Pseudomonas aeruginosa type III secretion system (T3SS).
Synthesis and structure-activity relationships of novel phenoxyacetamide inhibitors of the Pseudomonas aeruginosa type III secretion system (T3SS).
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DOI：
10.1016/j.bmc.2015.01.011
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发表时间：
2015-03-01
影响因子：
3.5
通讯作者：
Moir DT
中科院分区：
文献类型：
--
作者：
Williams JD;Torhan MC;Neelagiri VR;Brown C;Bowlin NO;Di M;McCarthy CT;Aiello D;Peet NP;Bowlin TL;Moir DT
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.
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影响因子：
11.4
作者：
Charles, PGP;Grayson, ML
通讯作者：
Grayson, ML
DOI：
10.1038/nrmicro2199
发表时间：
2009-09
期刊：
Nature reviews. Microbiology
影响因子：
--
作者：
通讯作者：
--
影响因子：
3.1
作者：
Milla, Carlos E.;Chmiel, James F.;Accurso, Frank J.;VanDevanter, Donald R.;Konstan, Michael W.;Yarranton, Geoffrey;Geller, David E.
通讯作者：
Geller, David E.
影响因子：
6.4
作者：
Roy-Burman, A;Savel, RH;Wiener-Kronish, JP
通讯作者：
Wiener-Kronish, JP
DOI：
10.1164/rccm.200802-239oc
发表时间：
2008-09-01
影响因子：
24.7
作者：
El Solh, Ali A.;Alkinnusi, Morohunfolu E.;Szarpa, Kristie
通讯作者：
Szarpa, Kristie