Synthesis and Antiparasitic Activity of New Conjugates—Organic Drugs Tethered to Trithiolato-Bridged Dinuclear Ruthenium(II)–Arene Complexes

Tethering known drugs to a metalorganic moiety is an efficient approach for modulating the anticancer, antibacterial, and antiparasitic activity of organometallic complexes. This study focused on synthesis evaluation new dinuclear ruthenium(II)–arene compounds linked several antimicrobial such as dapsone, sulfamethoxazole, sulfadiazine, sulfadoxine, triclosan, metronidazole, ciprofloxacin, well menadione (a 1,4-naphtoquinone derivative). In primary screen, 30 (17 hybrid molecules, diruthenium intermediates, antimicrobials) were assessed in vitro against transgenic T. gondii tachyzoites constitutively expressing β-galactosidase (T. β-gal) at 0.1 1 µM. parallel, cytotoxicity noninfected host cells (human foreskin fibroblasts, HFF) was determined by alamarBlue assay. When µM, five strongly impaired parasite proliferation >90%, HFF viability retained 50% or more, they further subjected β-gal dose-response studies. Two compounds, notably 11 13, amide ester conjugates with sulfadoxine exhibited low IC50 (half-maximal inhibitory concentration) values 0.063 0.152 intermediate impairment 2.5 µM (83 64%). The nature anchored drug that linking unit impacted biological activity.