Discovery of dual GyrB/ParE inhibitors active against Gram-negative bacteria

Discovery of dual GyrB/ParE inhibitors active against Gram-negative bacteria
Title:
Discovery of dual GyrB/ParE inhibitors active against Gram-negative bacteria
Other Titles:
European Journal of Medicinal Chemistry
Publication Date:
11 August 2018
Citation:
Soo Yei Ho, Weiling Wang, Fui Mee Ng, Yun Xuan Wong, Zhi Ying Poh, Sum Wai Eldwin Tan, Shi Hua Ang, Si Si Liew, Yin Sze Joyner Wong, Yvonne Tan, Anders Poulsen, Vishal Pendharkar, Kanda Sangthongpitag, John Manchester, Gregory Basarab, Jeffrey Hill, Thomas H. Keller, Joseph Cherian, Discovery of dual GyrB/ParE inhibitors active against Gram-negative bacteria, European Journal of Medicinal Chemistry, Volume 157, 2018, Pages 610-621, ISSN 0223-5234, https://doi.org/10.1016/j.ejmech.2018.08.025.
Abstract:
Even though many GyrB and ParE inhibitors have been reported in the literature, few possess activity against Gram-negative bacteria. This is primarily due to limited permeability across Gram-negative bacterial membrane as well as bacterial efflux mechanisms. Permeability of compounds across Gram-negative bacterial membranes depends on many factors including physicochemical properties of the inhibitors. Herein, we show the optimization of pyridylureas leading to compounds with potent activity against Gram-negative bacterial species such as P.aeruginosa, E.coli and A.baumannii.
License type:
http://creativecommons.org/licenses/by-nc-nd/4.0/
Funding Info:
Agency for Science, Technology and Research (A*STAR) Biomedical Research Council
Description:
ISSN:
0223-5234
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