Antimicrobial Activity of Some Steroidal Hydrazones
Maia Merlani,
Nanuli Nadaraia,
Lela Amiranashvili,
Anthi Petrou,
Athina Geronikaki,
Ana Ciric,
Jasmina Glamoclija,
Tamara Carevic,
Marina Sokovic
Affiliations
Maia Merlani
TSMU I. Kutateladze Institute of Pharmacochemistry, Tbilisi 0159, Georgia
Nanuli Nadaraia
TSMU I. Kutateladze Institute of Pharmacochemistry, Tbilisi 0159, Georgia
Lela Amiranashvili
TSMU I. Kutateladze Institute of Pharmacochemistry, Tbilisi 0159, Georgia
Anthi Petrou
School of Pharmacy, Aristotle University of Thessaloniki, 54124 Thessaloniki, Greece
Athina Geronikaki
School of Pharmacy, Aristotle University of Thessaloniki, 54124 Thessaloniki, Greece
Ana Ciric
Mycological Laboratory, Department of Plant Physiology, Institute for Biological Research “Siniša Stankovi’c”, University of Belgrade, 11060 Beograd, Serbia
Jasmina Glamoclija
Mycological Laboratory, Department of Plant Physiology, Institute for Biological Research “Siniša Stankovi’c”, University of Belgrade, 11060 Beograd, Serbia
Tamara Carevic
Mycological Laboratory, Department of Plant Physiology, Institute for Biological Research “Siniša Stankovi’c”, University of Belgrade, 11060 Beograd, Serbia
Marina Sokovic
Mycological Laboratory, Department of Plant Physiology, Institute for Biological Research “Siniša Stankovi’c”, University of Belgrade, 11060 Beograd, Serbia
Twelve steroid based hydrazones were in silico evaluated using computer program PASS as antimicrobial agents. The experimental evaluation revealed that all compounds have low to moderate antibacterial activity against all bacteria tested, except for B. cereus with MIC at a range of 0.37–3.00 mg/mL and MBC at 0.75–6.00 mg/mL. The most potent appeared to be compound 11 with MIC/MBC of 0.75/1.5 mg/mL, respectively. The evaluation of antibacterial activity against three resistant strains MRSA, E. coli and P. aeruginosa demonstrated superior activity of compounds against MRSA compared with ampicillin, which did not show bacteriostatic or bactericidal activities. All compounds exhibited good antifungal activity with MIC of 0.37–1.50 mg/mL and MFC of 1.50–3.00 mg/mL, but with different sensitivity against fungi tested. According to docking studies, 14-alpha demethylase inhibition may be responsible for antifungal activity. Two compounds were evaluated for their antibiofilm activity. Finally, drug-likeness and docking prediction were performed.
