title: Synthesis and biological evaluation of N-acylhydrazones as inhibitors of MurC and MurD ligases.
abstract: The Mur ligases have an essential role in the intracellular biosynthesis of bacterial peptidoglycan, and they represent attractive targets for the design of novel antibacterials. A series of compounds with an N-acylhydrazone scaffold were synthesized and screened for inhibition of the MurC and MurD enzymes from Escherichia coli. Compounds with micromolar inhibitory activities against both MurC and MurD were identified, and some of them also showed antibacterial activity.
authors.affiliation: University of Ljubljana, Faculty of Pharmacy, Askerceva 7, 1000 Ljubljana, Slovenia.
authors.forename: Roman
authors.initials: R
authors.lastname: Sink
authors.forename: Andreja
authors.initials: A
authors.lastname: Kovac
authors.forename: Tihomir
authors.initials: T
authors.lastname: Tomasić
authors.forename: Veronika
authors.initials: V
authors.lastname: Rupnik
authors.forename: Audrey
authors.initials: A
authors.lastname: Boniface
authors.forename: Julieanne
authors.initials: J
authors.lastname: Bostock
authors.forename: Ian
authors.initials: I
authors.lastname: Chopra
authors.forename: Didier
authors.initials: D
authors.lastname: Blanot
authors.forename: Lucija Peterlin
authors.initials: LP
authors.lastname: Masic
authors.forename: Stanislav
authors.initials: S
authors.lastname: Gobec
authors.forename: Anamarija
authors.initials: A
authors.lastname: Zega
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D001426:Bacterial Proteins / Q000037:antagonists & inhibitors / Q000737:chemistry; D018360:Crystallography, X-Ray; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D004926:Escherichia coli / Q000187:drug effects* / Q000201:enzymology; D006835:Hydrazones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D008025:Ligases / Q000037:antagonists & inhibitors* / Q000737:chemistry; D008826:Microbial Sensitivity Tests; D008958:Models, Molecular; D015394:Molecular Structure; D010457:Peptidoglycan / Q000096:biosynthesis; D013211:Staphylococcus aureus / Q000187:drug effects; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: D000900:Anti-Bacterial Agents; D001426:Bacterial Proteins; D004791:Enzyme Inhibitors; D006835:Hydrazones; D010457:Peptidoglycan; D008025:Ligases