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In vitro multitarget activity of sulfadiazine substituted triazenes as antimicrobial, cytotoxic, and larvicidal
Hasan Aydin1, Süleyman Akocak2, Nebih Lolak2
1Department of Pharmaceutical Toxicology, Faculty of Pharmacy, Adıyaman 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, 1 H-NMR, 13 C-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.
Insights
Novel sulfadiazine derivatives combat multidrug resistance (MDR). These multitargeted compounds show promising antibacterial, antifungal, antiviral, cytotoxic, and larvicidal activities, offering potential for new drug development against resistant infections and cancer.
Area of Science:
- Medicinal Chemistry
- Drug Discovery
- Antimicrobial Research
Background:
- Multidrug resistance (MDR) poses significant challenges in treating infections and cancer.
- Developing novel multitargeted drugs is crucial to overcome resistance and reduce treatment costs and toxicity.
- Existing treatments necessitate innovative strategies to combat the growing threat of drug resistance.
Purpose of the Study:
- To synthesize and evaluate novel 1,3-diaryltriazene-substituted sulfadiazine (SDZ) derivatives for multitargeted activities.
- To investigate the in vitro antibacterial, antifungal, antiviral, cytotoxic, and larvicidal effects of these new compounds.
- To identify potent lead compounds for next-generation therapeutic agents against drug-resistant conditions.
Main Methods:
- Synthesis of twelve novel 1,3-diaryltriazene-substituted SDZ derivatives.
- Characterization of synthesized compounds using spectroscopic (FT-IR, NMR) and analytical methods.
- In vitro evaluation of biological activities including antibacterial, antifungal, antiviral (Modified Vaccinia Virus Ankara), cytotoxic, and larvicidal (Lucilia sericata) assays.
Main Results:
- All twelve synthesized derivatives (AH1-12) demonstrated multitargeted potential.
- Derivative AH1 exhibited the strongest antibacterial and antifungal activity.
- Derivatives AH2, AH3, AH5, and AH7 displayed enhanced antiviral activity compared to SDZ.
- All derivatives showed superior cytotoxic and significant larvicidal activity at 72 hours.
Conclusions:
- The novel 1,3-diaryltriazene-substituted SDZ derivatives are effective multitargeted agents.
- These compounds represent promising leads for developing next-generation drugs to combat MDR in infectious diseases and cancer.
- Further research is warranted to explore their therapeutic potential and optimize their efficacy.
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