Antimicrobial Activity of Some Steroidal Hydrazones

Area of Science:

• Medicinal Chemistry
• Pharmacology
• Computational Chemistry

Background:

• Steroid-based hydrazones are explored for their potential as antimicrobial agents.
• In silico and experimental evaluations are crucial for identifying novel drug candidates.

Purpose of the Study:

• To evaluate twelve steroid-based hydrazones as antimicrobial and antifungal agents.
• To investigate the mechanism of action for antifungal activity using docking studies.
• To assess drug-likeness and antibiofilm potential.

Main Methods:

• In silico evaluation using the PASS program.
• Experimental determination of Minimum Inhibitory Concentration (MIC) and Minimum Bactericidal Concentration (MBC).
• Antifungal activity testing (MIC and MFC) and molecular docking for mechanism prediction.
• Antibiofilm activity assessment and drug-likeness prediction.

Main Results:

• Compounds showed low to moderate antibacterial activity, with notable efficacy against *Bacillus cereus* (MIC: 0.37-3.00 mg/mL).
• Compound 11 demonstrated significant potency against *B. cereus* (MIC/MBC: 0.75/1.5 mg/mL).
• Superior activity against Methicillin-resistant *Staphylococcus aureus* (MRSA) was observed compared to ampicillin.
• Good antifungal activity was recorded (MIC: 0.37-1.50 mg/mL), with 14-alpha demethylase inhibition suggested as the mechanism.
• Two compounds exhibited antibiofilm activity.

Conclusions:

• Steroid-based hydrazones possess significant antimicrobial and antifungal properties.
• Compound 11 and others show potential as therapeutic agents against resistant bacteria like MRSA.
• Inhibition of 14-alpha demethylase is a likely mechanism for the observed antifungal effects.