Chalcones and Their Heterocyclic Analogues as Potential Therapeutic Agents of Bacte-rial Diseases
Katedra farmaceutické chemie a kontroly léčiv Farmaceutické fakulty Univerzity Karlovy
Čes. slov. Farm., 2000; , 278-284
Chalcones and their heterocyclic analogues possess a number of biological effects. Their antifungaleffects 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. Forantibacterial activity, the presence of the enone aggregate in the molecule is important. Hydroge-nated analogues are less effective or ineffective, saturated brominated analogues are effectiveprobably after a metabolic transformation into unsaturated a-bromochalcone. In the rings, substi-tution 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 derivativesagainst gram-positive microorganisms is usually higher than against gram-negative bacteria. Someanalogues, however, inhibited also the growth of gram-negative strains. With regard to increasedincidence of tuberculosis in recent years, antimycobacterial effectiveness of chalcones and theirderivatives is especially interesting.
chalcones – heterocyclic analogues of chalcones – antibacterial activity– antimycobacterial activity
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