title: Creating an antibacterial with in vivo efficacy: synthesis and characterization of potent inhibitors of the bacterial cell division protein FtsZ with improved pharmaceutical properties.
abstract: 3-Methoxybenzamide (1) is a weak inhibitor of the essential bacterial cell division protein FtsZ. Alkyl derivatives of 1 are potent antistaphylococcal compounds with suboptimal drug-like properties. Exploration of the structure-activity relationships of analogues of these inhibitors led to the identification of potent antistaphylococcal compounds with improved pharmaceutical properties.
authors.affiliation: Biota Europe Ltd., Begbroke Science Park, Yarnton, Oxfordshire, UK. d.haydon@biota.com.au
authors.forename: David J
authors.initials: DJ
authors.lastname: Haydon
authors.forename: James M
authors.initials: JM
authors.lastname: Bennett
authors.forename: David
authors.initials: D
authors.lastname: Brown
authors.forename: Ian
authors.initials: I
authors.lastname: Collins
authors.forename: Greta
authors.initials: G
authors.lastname: Galbraith
authors.forename: Paul
authors.initials: P
authors.lastname: Lancett
authors.forename: Rebecca
authors.initials: R
authors.lastname: Macdonald
authors.forename: Neil R
authors.initials: NR
authors.lastname: Stokes
authors.forename: Pramod K
authors.initials: PK
authors.lastname: Chauhan
authors.forename: Jignesh K
authors.initials: JK
authors.lastname: Sutariya
authors.forename: Narendra
authors.initials: N
authors.lastname: Nayal
authors.forename: Anil
authors.initials: A
authors.lastname: Srivastava
authors.forename: Joy
authors.initials: J
authors.lastname: Beanland
authors.forename: Robin
authors.initials: R
authors.lastname: Hall
authors.forename: Vincent
authors.initials: V
authors.lastname: Henstock
authors.forename: Caterina
authors.initials: C
authors.lastname: Noula
authors.forename: Chris
authors.initials: C
authors.lastname: Rockley
authors.forename: Lloyd
authors.initials: L
authors.lastname: Czaplewski
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001426:Bacterial Proteins / Q000037:antagonists & inhibitors*; D001682:Biological Availability; D001798:Blood Proteins / Q000378:metabolism; D018938:Caco-2 Cells; D002455:Cell Division / Q000187:drug effects; D002463:Cell Membrane Permeability; D003598:Cytoskeletal Proteins / Q000037:antagonists & inhibitors*; D022781:Hepatocytes / Q000378:metabolism; D006801:Humans; D051379:Mice; D008826:Microbial Sensitivity Tests; D008958:Models, Molecular; D011485:Protein Binding; D011725:Pyridines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013203:Staphylococcal Infections / Q000188:drug therapy; D013211:Staphylococcus aureus / Q000166:cytology / Q000187:drug effects*; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
chemical_list: D000900:Anti-Bacterial Agents; D001426:Bacterial Proteins; D001798:Blood Proteins; D003598:Cytoskeletal Proteins; C071525:FtsZ protein, Bacteria; C531944:PC190723; D011725:Pyridines; D013844:Thiazoles