title: Tyrosyl-tRNA synthetase inhibitors: a patent review.
abstract: Bacterial infection has been a consistent and relentless threat to human health because of emerging resistance to existing antibiotics. Therefore, much of the research has been focused on the design of new potent antibacterial agents. Tyrosyl-tRNA synthetase (TyrRS), as a member of aminoacyl-tRNA synthetase family, could recognize the information including the coincident tRNA molecules and the amino acids' structures, which are essential in translating the coded information into protein structures in nucleic acids. Therefore, the discovery and application of tyrosyl-tRNA synthetase inhibitors might be a potential strategy to control these diseases in humans. Areas covered: This review covers 1999 to 2016 wherein several new analogues were claimed as TyrRS inhibitors based on their chemical structures. Xiao, Z.P. et al patented two Chinese patents related to TyrRS inhibitors which are included. Expert opinion: Due to the pivotal role in translation, tyrosyl-tRNA synthetase has been recognized as a promising target for a new generation of antibiotics with selectivity and specificity. However, while some of the TyrRS inhibitors showed encouraging results, there is an urgent need to develop novel TyrRS inhibitors with higher activity and selectivity. Based on the published SAR results, selective tyrosyl-tRNA synthetase inhibitors could be designed and developed as the next generation of antibacterial agents.
authors.affiliation: a State Key Laboratory of Pharmaceutical Biotechnology , Nanjing University , Nanjing , PR China.|b School of Life Sciences , Shandong University of Technology , Zibo , PR China.
authors.forename: Juan
authors.initials: J
authors.lastname: Sun
authors.affiliation: a State Key Laboratory of Pharmaceutical Biotechnology , Nanjing University , Nanjing , PR China.
authors.forename: Peng-Cheng
authors.initials: PC
authors.lastname: Lv
authors.affiliation: a State Key Laboratory of Pharmaceutical Biotechnology , Nanjing University , Nanjing , PR China.|b School of Life Sciences , Shandong University of Technology , Zibo , PR China.
authors.forename: Hai-Liang
authors.initials: HL
authors.lastname: Zhu
mesh_terms: D000900:Anti-Bacterial Agents / Q000737:chemistry / Q000494:pharmacology*; D001419:Bacteria / Q000187:drug effects / Q000201:enzymology; D001424:Bacterial Infections / Q000188:drug therapy* / Q000382:microbiology; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D010330:Patents as Topic; D013329:Structure-Activity Relationship; D014448:Tyrosine-tRNA Ligase / Q000037:antagonists & inhibitors* / Q000378:metabolism
chemical_list: D000900:Anti-Bacterial Agents; D004791:Enzyme Inhibitors; D014448:Tyrosine-tRNA Ligase
keywords: TyrRS; adenosine; antibacterial agents; arylfuran; inhibitors; metronidazole