Structural highlights
Function
[G6JAH7_STREE] Topoisomerase IV is essential for chromosome segregation. It relaxes supercoiled DNA. Performs the decatenation events required during the replication of a circular DNA molecule.[HAMAP-Rule:MF_00939]
Publication Abstract from PubMed
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.
Discovery of dual GyrB/ParE inhibitors active against Gram-negative bacteria.,Ho SY, Wang W, Ng FM, Wong YX, Poh ZY, Tan SWE, Ang SH, Liew SS, Joyner Wong YS, Tan Y, Poulsen A, Pendharkar V, Sangthongpitag K, Manchester J, Basarab G, Hill J, Keller TH, Cherian J Eur J Med Chem. 2018 Aug 11;157:610-621. doi: 10.1016/j.ejmech.2018.08.025. PMID:30125722[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
See Also
References
- ↑ Ho SY, Wang W, Ng FM, Wong YX, Poh ZY, Tan SWE, Ang SH, Liew SS, Joyner Wong YS, Tan Y, Poulsen A, Pendharkar V, Sangthongpitag K, Manchester J, Basarab G, Hill J, Keller TH, Cherian J. Discovery of dual GyrB/ParE inhibitors active against Gram-negative bacteria. Eur J Med Chem. 2018 Aug 11;157:610-621. doi: 10.1016/j.ejmech.2018.08.025. PMID:30125722 doi:http://dx.doi.org/10.1016/j.ejmech.2018.08.025
