Supriya Mahajan

Triazine derivatives were reported to show a wide range of biological activities. Hence, it was planned to perform docking studies, synthesize and screen these designed compounds for their in vivo anti-inflammatory activity. In order to study the interaction of ligands with the binding site of the enzyme, the triazine derivatives were docked on cyclooxygenase-2 (COX-2) enzyme using the drug design software Maestro 9.5, Schrodinger, USA. The series of 8 compounds showing good Glide score (G-score) was synthesized to form 4-anilinoquinoline triazines. The structures of the compounds were confirmed by IR, 1H NMR and mass spectroscopy and the compounds were screened for anti-inflammatory activity by carrageenan- induced rat hind paw edema method, using Diclofenac as the standard. The G-scores of all the 8 compounds were closer to the scores displayed by the standard drugs, celecoxib and SC-558, there by suggesting that all the compounds interacted very well with the COX-2 enzyme. The in vivo anti-inflammatory activity results revealed that all the compounds displayed % inhibition of edema more than 90, which was better than that shown by the standard drug, Diclofenac. Amongst all the compounds, 3b demonstrated the highest G-score as well as the highest anti-inflammatory activity. Hence, this compound may be explored as a potential lead molecule for further development.

Sulfones are known to possess various biological activities. Their great potential as bioactive compounds, combined with the easy method of synthesis, make this class a strong candidate for the production of medicines economically. This article deals with the synthesis of a series of ten diaryl sulfones, their antibacterial activity, individually, synergistic antibacterial activity with trimethoprim against E. coli and preliminary QSAR studies. The antibacterial activity was performed by agar diffusion method, against Gram positive and Gram negative bacteria. Few derivatives exhibited antibacterial activity comparable to or better than the standard, sulphamethoxazole, against Gram negative organisms (E. coli and S. dysentrae). Sulfones being folic acid inhibitors, their synergistic effect was checked with trimethoprim on E. coli. Most of the compounds exhibited synergistic effect with trimethoprim, which was better than the combination of trimethoprim and sulfamethoxazole (1:5). Quantitative structure activity relationships studies were performed by multiple linear regression analysis. The antibacterial activity of sulfones was found to correlate well with their dipole moment and ionization potential.