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Current Perspectives on Biological Screening of Newly Synthetised Sulfanilamide Schiff Bases as Promising Antibacterial and Antibiofilm Agents

2024; Multidisciplinary Digital Publishing Institute; Volume: 17; Issue: 4 Linguagem: Inglês

10.3390/ph17040405

1424-8247

Maria Coandă, Carmen Limban, Constantin Drăghici, Anne-Marie Ciobanu, Georgiana Alexandra Grigore, Marcela Popa, Miruna S. Stan, Cristina Larion, Speranța Avram, Cătălina Mareş, M C Ciornei, Aura Dabu, Ariana Hudiță, Bianca Gălățeanu, Lucia Pintilie, Diana Camelia Nuță,

Enzyme function and inhibition

Growing resistance to antimicrobials, combined with pathogens that form biofilms, presents significant challenges in healthcare. Modifying current antimicrobial agents is an economical approach to developing novel molecules that could exhibit biological activity. Thus, five sulfanilamide Schiff bases were synthesized under microwave irradiation and characterized spectroscopically and in silico. They were evaluated for their antimicrobial and antibiofilm activities against both Gram-positive and Gram-negative bacterial strains. Their cytotoxic potential against two cancer cell lines was also determined. Gram-positive bacteria were susceptible to the action of these compounds. Derivatives 1b and 1d inhibited S. aureus’s growth (MIC from 0.014 mg/mL) and biofilm (IC from 0.029 mg/mL), while compound 1e was active against E. faecalis’s planktonic and sessile forms. Two compounds significantly reduced cell viability at 5 μg/mL after 24 h of exposure (1d—HT-29 colorectal adenocarcinoma cells, 1c—LN229 glioblastoma cells). A docking study revealed the increased binding affinities of these derivatives compared to sulfanilamide. Hence, these Schiff bases exhibited higher activity compared to their parent drug, with halogen groups playing a crucial role in both their antimicrobial and cytotoxic effects.