By 2050 {it is|it’s|it really is|it truly is|it can be|it is actually} predicted that antimicrobial resistance {will be|will probably be|will likely be|is going to be|might be|are going to be} {responsible|accountable} for {10|ten} million {global|international|worldwide} deaths annually, costing the {world|globe|planet} economy $100 trillion. Clearly, {strategies|methods|techniques|approaches|tactics} to address this {problem|issue|difficulty|dilemma|challenge|trouble} are {required|needed|necessary|essential|expected} as bacterial evolution is rendering our {current|present|existing} antibiotics ineffective. The discovery of an allosteric binding {site|website|web site|internet site|web-site|web page} {on the|around the} established antibacterial target DNA gyrase {offers|provides|gives|delivers|presents} {a new|a brand new} medicinal chemistry {strategy|technique|method|approach|tactic}, as this {site|website|web site|internet site|web-site|web page} is distinct {from the|in the} fluoroquinolone-DNA {site|website|web site|internet site|web-site|web page} binding {site|website|web site|internet site|web-site|web page}. {Using|Utilizing|Making use of|Employing|Working with|Applying} in silico molecular {design|style|design and style} {methods|techniques|strategies|approaches|procedures|solutions}, {we have|we’ve|we’ve got} {designed|developed|created|made} and synthesised a novel series of biphenyl-based inhibitors inspired by the published thiophene allosteric inhibitor. This series was evaluated in vitro against E. coli DNA gyrase, exhibiting IC50 values {in the|within the|inside the} low micromolar {range|variety}. The structure-activity {relationship|partnership|connection} reported herein suggests insights to {further|additional} exploit this allosteric {site|website|web site|internet site|web-site|web page}, {offering|providing|supplying} a pathway to overcome fluoroquinolone resistance. 13315-17-8 Chemical name 23405-32-5 supplier PMID:23613863
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