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  Česky / Czech version Čes. a slov. Farm. 49, 2000, No. 6, p. 278–284
 
Chalcones and Their Heterocyclic Analogues as Potential Therapeutic Agents of Bacte- rial Diseases 
OPLETALOVÁ V. 

Katedra farmaceutické chemie a kontroly léčiv Farmaceutické fakulty Univerzity Karlovy,
 


Summary:

       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, 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 amino groups 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.

        Key words: chalcones – heterocyclic analogues of chalcones – antibacterial activity – antimycobacterial activity
       

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