Identification and Structure?Activity Relationships of Novel Compounds that Potentiate the Activities of Antibiotics in Escherichia coli [electronic resource]

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Tác giả:

Ngôn ngữ: eng

Ký hiệu phân loại: 541 Physical chemistry

Thông tin xuất bản: Oak Ridge, Tenn. : Distributed by the Office of Scientific and Technical Information, U.S. Dept. of Energy, 2017

Mô tả vật lý: Size: p. 6205-6219 : , digital, PDF file.

Bộ sưu tập: Metadata

ID: 260467

In Gram-negative bacteria, efflux pumps are able to prevent effective cellular concentrations from being achieved for a number of antibiotics. Small molecule adjuvants that act as efflux pump inhibitors (EPIs) have the potential to reinvigorate existing antibiotics that are currently ineffective due to efflux mechanisms. Through a combination of rigorous experimental screening and in silico virtual screening, we recently identified novel classes of EPIs that interact with the membrane fusion protein AcrA, a critical component of the AcrAB-TolC efflux pump in Escherichia coli. In this paper, we present initial optimization efforts and structure?activity relationships around one of those previously described hits, NSC 60339 (1). Finally, from these efforts we identified two compounds, SLUPP-225 (17h) and SLUPP-417 (17o), which demonstrate favorable properties as potential EPIs in E. coli cells including the ability to penetrate the outer membrane, improved inhibition of efflux relative to 1, and potentiation of the activity of novobiocin and erythromycin.
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