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In vitro multitarget activity of sulfadiazine substituted triazenes as antimicrobial,cytotoxic, and larvicidal agents
Authors:Hasan Aydin  Süleyman Akocak  Nebih Lolak  Uğur Uslu  Ahmet Sait  Serol Korkmaz  Ayşe Parmaksiz  Onur Ceylan  Abdulbaki Aksakal
Institution:1. Department of Pharmaceutical Toxicology, Faculty of Pharmacy, Adıyaman University, Adıyaman, Türkiye;2. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Adıyaman University, Adıyaman, Türkiye;3. Department of Medical Microbiology, Faculty of Medicine, Selçuk University, Konya, Türkiye;4. Virology Laboratory of Pendik Veterinary Control Institute, İstanbul, Türkiye;5. Department of Parasitology, Faculty of Veterinary Medicine, Selçuk University, Konya, Türkiye;6. Department of Pharmaceutical Microbiology, Faculty of Pharmacy, Adiyaman University, Adıyaman, Türkiye
Abstract:Multidrug resistance (MDR) causes difficulties in the treatment of infections and cancer. Research and development studies have become increasingly important for the strategy of preventing MDR. There is a need for new multitarget drug research and advancement to reduce the development of drug resistance in drug-drug interactions and reduce cost and toxic effects. This study aimed to determine the effects of multi-target triazene compounds on antibacterial, antifungal, antiviral, cytotoxic, and larvicidal activities were investigated in vitro. A series of 12 novel of 1,3-diaryltriazene-substituted sulfadiazine (SDZ) derivatives were synthesized, and the obtained pure products characterized in detail by spectroscopic and analytic methods (FT-IR, 1H-NMR, 13C-NMR, and melting points). The antibacterial and antifungal activities of these derivatives (AH1-12) were determined by broth microdilution method. All derivatives have been evaluated in cell-based assays for cytotoxic and antiviral activities against Modified Vaccinia Virus Ankara. The larvicidal efficacy of these chemical compounds was also investigated by using Lucilia sericata (L. sericata) larvae. Twelve 1,3-diaryltriazene-substituted SDZ derivatives (AH1-12) were designed and developed as potent multitargeted compounds. Among them, the AH1 derivative showed the most antibacterial and antifungal activity. Besides, synthesized derivatives AH2, AH3, AH5, and AH7 showed higher antiviral activity than SDZ. All synthesized derivatives showed higher cytotoxic activity than SDZ. Also, they showed larvicidal activity at 72 h of the experiment. As a result, these compounds might be great leads for the development of next-generation multitargeted agents.
Keywords:1  3-diaryl triazenes  antibacterial  antifungal  antiviral activity  sulfa drugs
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