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

Author:

Coanda Maria1,Limban Carmen1,Draghici Constantin2,Ciobanu Anne-Marie3ORCID,Grigore Georgiana Alexandra456,Popa Marcela45,Stan Miruna4ORCID,Larion Cristina5,Avram Speranta7,Mares Catalina7ORCID,Ciornei Mariana-Catalina8,Dabu Aura9,Hudita Ariana45ORCID,Galateanu Bianca45,Pintilie Lucia10ORCID,Nuta Diana Camelia1ORCID

Affiliation:

1. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Carol Davila University of Medicine and Pharmacy, 6 Traian Vuia Str., 020950 Bucharest, Romania

2. Costin D. Nenitzescu Institute of Organic and Supramolecular Chemistry, 202 B Splaiul Independentei, 060023 Bucharest, Romania

3. Department of Drug Control, Faculty of Pharmacy, Carol Davila University of Medicine and Pharmacy, 6 Traian Vuia Str., 020950 Bucharest, Romania

4. Faculty of Biology, University of Bucharest, Splaiul Independenței 91-95, 050095 Bucharest, Romania

5. Research Institute of the University of Bucharest (ICUB), University of Bucharest, Șoseaua Panduri 90, 050663 Bucharest, Romania

6. National Institute Research and Development for Biological Sciences, Splaiul Independenței 296, 060031 Bucharest, Romania

7. Department of Anatomy, Animal Physiology and Biophysics, Faculty of Biology, University of Bucharest, Splaiul Independentei 91-95, 050095 Bucharest, Romania

8. Physiology Department, Carol Davila University of Medicine and Pharmacy, 020021 Bucharest, Romania

9. Neurosurgery Department 1, The University Emergency Hospital of Bucharest, Splaiul Independenței 169, 050098 Bucharest, Romania

10. National Institute for Chemical-Pharmaceutical Research and Development, 112 Vitan Av., 031299 Bucharest, Romania

Abstract

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.

Funder

Ministry of Research, Innovation and Digitization, CNCS UEFISCDI

Publisher

MDPI AG

Reference53 articles.

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