Antimicrobial, anti-TB, anticancer and anti-HIV evaluation of new s-triazine-based heterocycles.

BACKGROUND: The acquirement of resistance by microorganisms to the antimicrobial arsenal is a threat to public health. A recent WHO report estimated that 1.3 million HIV-negative people and 0.38 million HIV-positive people died from TB in 2009. Various forms of cancer account for a high percentage of deaths in both women (breast cancer) and men (prostate cancer). RESULTS & DISCUSSION: In vitro activity assessment of newly constructed s-triazines against a panel of microorganisms including bacteria, fungi and Mycobacteria demonstrated that the compounds are of immense attraction for impending drug discovery. They were further examined for in vitro activity against breast cancer and prostate cancer cell lines, as well as HIV-1 (III(B)) and HIV-2 (ROD) viral strains. Proposed structural confirmation studies by IR, (1)H NMR, (13)C NMR, (19)F NMR spectroscopy and elemental analysis were in accordance. CONCLUSION: Activity profiles of the products may contribute considerably to future drug-discovery studies.

Synthesis and studies of new 2-(coumarin-4-yloxy)-4,6-(substituted)-S-triazine derivatives as potential anti-HIV agents.

Novel 2-(coumarin-4-yloxy)-4,6-(substituted)-s-triazine derivatives i. e., diaryltriazine (DATA) are reported as novel non-nucleoside reverse transcriptase inhibitors (NNRTIs), were synthesized and their activities against human immunodeficiency virus HIV-1 (III-B), HIV-2 (ROD), and the double RT mutant HIV-1 (K103N and Y181C) were assessed. Modifications at positions 4 and 6 of the coumarinyl-triazine scaffold generated interesting derivatives displaying good to moderate anti-HIV activity against selected HIV strains as compared to nevirapine and efavirenz. The synthesized compounds were characterized by FTIR, (1)H-NMR, and mass spectral data together with elemental analysis.