1. THIOUREA DERIVATIVES OF 4-AZATRICYCLO[5.2.2.0(2.6)]UNDEC-8-ENE-3,5 DIONE - SYNTHESIS AND BIOLOGICAL ACTIVITY.
- Author
-
Bielenica A, Stefańska J, Kozioł AE, Iuliano F, Collu D, Sanna G, Jóźwiak M, and Struga M
- Subjects
- Crystallography, X-Ray, Drug Screening Assays, Antitumor, Gram-Positive Bacteria drug effects, Humans, Magnetic Resonance Spectroscopy, Microbial Sensitivity Tests, Models, Molecular, Thiourea pharmacology, Anti-Bacterial Agents chemical synthesis, Anti-Bacterial Agents pharmacology, Heterocyclic Compounds, 3-Ring chemical synthesis, Heterocyclic Compounds, 3-Ring pharmacology, Thiourea analogs & derivatives, Thiourea chemical synthesis
- 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.
- Published
- 2016