Structure-biological activity relationship of synthetic trihydroxilated chalcones

Abstract

The bacteriostatic activity of 2’,4’,2-trihydroxychalcone; 2’,4’,3-trihydroxychalcone and 2’,4’,4-trihydroxychalcone, prepared by condensation of 2,4-dihydroxyacetophenone and benzaldehyde substituted, against Staphylococcus aureus ATCC 25923 was assayed by agar plate method. The three compounds presented important inhibition halos. In order to elucidate structure-activity relationships, the minimal inhibitory concentrations against S. aureus were determined by the broth dilution method and the results obtained were compared to that of 2',4'-dihydroxychalcone. The sequence observed was: MIC 2’,4’,3-(OH)3 > MIC 2’,4’-(OH)2 > MIC 2’,4’,4-(OH)3 > > MIC 2’,4’,2-(OH)3. These results showed that the introduction of an electron donating group (-OH) in the aromatic B-ring causes an increase in bioactivity, and that the intensity of action depends on the position of the OH substitute.

Solvent-free synthesis, spectral correlations and antimicrobial activities of some aryl E 2-propen-1-ones

“…The Quantitative structure activity relationship and quantitative structure property relationships were used for finding the structure of molecule, quantitative and qualitative analysis [27][28][29]. Their use in structure parameter correlations becomes popular for studying biological activities [30], normal co-ordinate analysis [31] and transition states of reaction mechanisms [32]. Infrared spectroscopy is a powerful tool technique for the qualitative and quantitative study of natural and synthetic molecules [33].…”

Chalcones from Myracrodruon urundeuva are efficacious in guinea pig ovalbumin-induced allergic conjunctivitis

“…Chalcones are flavonoid analogues documented to possess a number of activities, such as antimicrobial, antiviral, antioxidant, antiprotozoal, anticancer, gastroprotective, and anti-inflammatory and analgesic properties (Devia et al, 1998;Opletalová et al, 2000;Calliste et al, 2001;Liu et al, 2001; Machala et al, Figure 5. Chalcones (Chalc, µg/mL) inhibit the myeloperoxidase release from human neutrophils in vitro.…”

Spectral Correlations and Antimicrobial Activities of some 1-Pyrenyl Chalcones

“…Chalcones possess various biological activities such as antibacterial [26,34], antifungal [26], antioxidant [8], antiviral [9], antimalarial [10], antiplasmodial [28], antituberclosis [12], antiproliferative [13], antileshmanial [14], anti-inflammatory [15], antianalgesic and sedative [16], insect antifeedants [13,22]. Halogenated chalcones possess insect antifeedant activities [13,22,42].…”