title: Combinatorial synthesis of substituted 3-(2-indolyl)piperidines and 2-phenyl indoles as inhibitors of ZipA-FtsZ interaction.
abstract: The ZipA-FtsZ protein-protein interaction is a potential target for antibacterial therapy. The design and parallel synthesis of a combinatorial library of small molecules, which target the FtsZ binding area on ZipA are described. Compounds were demonstrated to bind to the FtsZ binding domain of ZipA by HSQC NMR and to inhibit cell division in a cell elongation assay.
authors.affiliation: Wyeth Research, Department of Medicinal Chemistry, 401 N. Middletown Road, Pearl River, NY 10965, USA. jenninl@wyeth.com <jenninl@wyeth.com>
authors.forename: Lee D
authors.initials: LD
authors.lastname: Jennings
authors.forename: Kenneth W
authors.initials: KW
authors.lastname: Foreman
authors.forename: Thomas S
authors.initials: TS
authors.lastname: Rush
authors.forename: Desiree H H
authors.initials: DH
authors.lastname: Tsao
authors.forename: Lidia
authors.initials: L
authors.lastname: Mosyak
authors.forename: Scott L
authors.initials: SL
authors.lastname: Kincaid
authors.forename: Mohani N
authors.initials: MN
authors.lastname: Sukhdeo
authors.forename: Alan G
authors.initials: AG
authors.lastname: Sutherland
authors.forename: Weidong
authors.initials: W
authors.lastname: Ding
authors.forename: Cynthia Hess
authors.initials: CH
authors.lastname: Kenny
authors.forename: Chantel L
authors.initials: CL
authors.lastname: Sabus
authors.forename: Hanlan
authors.initials: H
authors.lastname: Liu
authors.forename: Elizabeth G
authors.initials: EG
authors.lastname: Dushin
authors.forename: Soraya L
authors.initials: SL
authors.lastname: Moghazeh
authors.forename: Pornpen
authors.initials: P
authors.lastname: Labthavikul
authors.forename: Peter J
authors.initials: PJ
authors.lastname: Petersen
authors.forename: Margareta
authors.initials: M
authors.lastname: Tuckman
authors.forename: Steven A
authors.initials: SA
authors.lastname: Haney
authors.forename: Alexey V
authors.initials: AV
authors.lastname: Ruzin
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D002352:Carrier Proteins / Q000737:chemistry*; D018797:Cell Cycle Proteins / Q000737:chemistry*; D002455:Cell Division / Q000187:drug effects; D020650:Combinatorial Chemistry Techniques; D004926:Escherichia coli / Q000166:cytology / Q000187:drug effects; D029968:Escherichia coli Proteins / Q000737:chemistry*; D007211:Indoles / Q000138:chemical synthesis* / Q000494:pharmacology; D020128:Inhibitory Concentration 50; D010880:Piperidines / Q000138:chemical synthesis* / Q000494:pharmacology; D011485:Protein Binding / Q000187:drug effects; D013329:Structure-Activity Relationship
chemical_list: D000900:Anti-Bacterial Agents; D002352:Carrier Proteins; D018797:Cell Cycle Proteins; D029968:Escherichia coli Proteins; C076835:FtsZ84 protein, E coli; D007211:Indoles; D010880:Piperidines; C103795:ZipA protein, E coli