Čes. slov. farm. 2000, 49(6):278-284
Chalcones and Their Heterocyclic Analogues as Potential Therapeutic Agents of Bacterial Diseases
- Katedra farmaceutické chemie a kontroly léčiv Farmaceutické fakulty Univerzity Karlovy
Chalcones and their heterocyclic analogues possess a number of biological effects. Their antifungal effects were reported in the previous communication (Opletalová V., Šedivý D.: Čes. a Slov. Farm.48, 252 (1999)). The present review is devoted to the antibacterial activity of these compounds. For antibacterial activity, the presence of the enone aggregate in the molecule is important. Hydroge-nated analogues are less effective or ineffective, saturated brominated analogues are effective probably after a metabolic transformation into unsaturated a-bromochalcone. In the rings, substitution with a hydroxyl is advantageous, in some cases also substitution with a lipophilic substituent,e.g. a halogen or an alkyl, proved to be advantageous. On the other hand, substitution with aminogroups often results in a decrease in effectiveness. Effectiveness of chalcones and their derivatives against gram-positive microorganisms is usually higher than against gram-negative bacteria. Some analogues, however, inhibited also the growth of gram-negative strains. With regard to increased incidence of tuberculosis in recent years, antimycobacterial effectiveness of chalcones and their derivatives is especially interesting.
Keywords: chalcones; heterocyclic analogues of chalcones; antibacterial activity; antimycobacterial activity
Published: June 1, 2000 Show citation