A series of novel xanthone conjugated amino acids were synthesised and characterised by analytical and spectroscopic methods. All the synthesized analogues () were screened for their antimicrobial and anti-inflammatory activities. Compounds, ,, ,, ,, and showed excellent antimicrobial activities compared to antibacterial and antifungal reference drugs gentamicin and bavistin, respectively. Compounds and showed good anti-inflammatory activity compared to a standard drug, indomethacin. The preliminary structure-activity relationship revealed that tryptophan, tyrosine, phenylalanine, proline and cysteine conjugated compounds showed excellent antimicrobial and anti-inflammatory activities. This may be explained by the contribution of aromaticity and hydrophobicity of amino acids. Molecular docking studies were performed for all the synthesised compounds, among which compounds , and showed the highest docking scores for antimicrobial activity while compounds, and showed the highest docking scores for anti-inflammatory activity. Different amino acids conjugated xanthone derivatives were synthesized and evaluated for their biological activities. The conjugation was found to play a major role in improving the biological activities of those compounds.
A series of new benzo[]thiazole-hydrazones were synthesized and characterized by analytical and spectroscopic techniques. All the compounds were screened for their inhibition of H/K ATPase and anti-inflammatory effects. The results revealed that compounds ,, ,, and displayed excellent inhibitory activity against H/K ATPase, and their IC values were lower than those of the standard compound omeprazole. Compounds ,, and exhibited better anti-inflammatory activity in comparison to the standard compound indomethacin. Studies of the structure-activity relationship (SAR) showed that electron-donating groups (OH and OCH) favored inhibitory activity against H/K ATPase, whereas electron-withdrawing groups (F, Cl, Br and NO) favored anti-inflammatory activity, and derivatives with both electron-donating (OH and OCH) and electron-withdrawing (Br) groups () displayed reasonable activity, whereas aliphatic analogues () exhibited less activity and heterocyclic analogues () displayed moderate activity in both biological studies. Molecular docking studies were performed for all the synthesized compounds, among which compounds and exhibited the highest docking scores for inhibitory activity against H/K ATPase, whereas compounds and displayed the highest docking scores for anti-inflammatory activity.
Amino acids conjugated with heterocyclic molecules are well known for their effective bioactive properties. In search of effective anticancer agents, a series of xanthone linked amino acids 2-23 were synthesized and tested for in vitro anticancer and DNA binding studies against three different cancer cell lines MCF-7, MDA-MB-435 and A549 and validated by DNA binding and molecular docking approaches. Compounds 7, 8 and 9 exhibited potent anticancer activity against tested cancer cell lines and DNA binding study using methyl green comparing to Doxorubicin and ethidium bromide as a positive control respectively. The structure-activity relationship (SAR) showed that the aromatic and hydrophobic amino acids (phenylalanine, tyrosine, and tryptophan) favoured the DNA binding studies and anticancer activity whereas, aliphatic amino acids showed least anticancer activity. In the molecular docking study, binding interactions of the most active compounds 7, 8 and 9 were confirmed to molecular surface of DNA is represented as Adenine (green), Thymine (red), Guanine (yellow) and Cytosine (blue) in respective colours.
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