title: THIOUREA DERIVATIVES OF 4-AZATRICYCLO[5.2.2.0(2.6)]UNDEC-8-ENE-3,5 DIONE - SYNTHESIS AND BIOLOGICAL ACTIVITY.
abstract: A series of halogeno derivatives of thiourea bearing a polycyclic imide core has been efficiently synthesized and evaluated for antimicrobial activity. The structures of the compounds were established by 1H and 13C NMR and MS methods. The molecular structure of 4Clc was determined by an X-ray crystallography. Compounds containing 3-chloro-4-fluorophenyl substituent (3Cl4Fb, 3Cl4Fd) were found to be the most promising against Gram-positive bacteria (MIC values ranged from 8 to 32 pg/mL for standard and 32 - 64 µg/mL for hospital strains). The in vitro cytotoxicity against MT-4 cells of all compounds was evaluated.
authors.forename: Anna
authors.initials: A
authors.lastname: Bielenica
authors.forename: Joanna
authors.initials: J
authors.lastname: Stefańska
authors.forename: Anna E
authors.initials: AE
authors.lastname: Kozioł
authors.forename: Filippo
authors.initials: F
authors.lastname: Iuliano
authors.forename: David
authors.initials: D
authors.lastname: Collu
authors.forename: Guseppina
authors.initials: G
authors.lastname: Sanna
authors.forename: Michał
authors.initials: M
authors.lastname: Jóźwiak
authors.forename: Marta
authors.initials: M
authors.lastname: Struga
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D018360:Crystallography, X-Ray; D004354:Drug Screening Assays, Antitumor; D006094:Gram-Positive Bacteria / Q000187:drug effects; D006575:Heterocyclic Compounds, 3-Ring / Q000138:chemical synthesis* / Q000494:pharmacology*; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D008826:Microbial Sensitivity Tests; D008958:Models, Molecular; D013890:Thiourea / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: C000609928:4-azatricyclo(5.2.2.0(2,6))undec-8-ene-3,5 dione; D000900:Anti-Bacterial Agents; D006575:Heterocyclic Compounds, 3-Ring; D013890:Thiourea