Morpholine Based Diazenyl Chalcones: Synthesis, Antimicrobial Screening and Cytotoxicity Study.

Area of Science:

• Medicinal Chemistry
• Microbiology
• Drug Discovery

Background:

• Microbial infections remain a significant global health challenge.
• Chalcone derivatives and morpholine compounds show promise as antimicrobial agents.
• Hybridizing these structures offers a novel approach to developing new antimicrobials.

Purpose of the Study:

• To synthesize and characterize a new series of morpholine-based heterocyclic diazenyl chalcones (MD1-MD21).
• To evaluate the antimicrobial potential of these novel compounds against various microbial strains.
• To assess the cytotoxicity and hemotoxicity of the most active derivatives.

Main Methods:

• Synthesis and characterization of 21 morpholine-based diazenyl chalcones.
• Antimicrobial activity evaluation using tube dilution and agar diffusion assays.
• Cytotoxicity testing on L929 and A549 cell lines; hemotoxicity assessment on human red blood cells.

Main Results:

• Compound MD-6 demonstrated high activity against *S. typhi, E. coli, A. niger*, and *C. albicans* (MIC: 1.95–3.91 µg/ml).
• MD-9 and MD-21 also exhibited significant antimicrobial effects.
• The most active compounds showed low cytotoxicity (IC50 > 35.42 µg/ml) and minimal hemolysis (0.2–5.5% at antimicrobial concentrations).

Conclusions:

• MD-6, MD-9, and MD-21 are potent antimicrobial agents.
• These derivatives possess a favorable safety profile with low cytotoxicity and hemotoxicity.
• The study highlights the potential of these novel compounds for developing new antimicrobial therapies.