Romanian Society of Pharmaceutical Sciences
 

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ANTI-BIOFILM ACTIVITY EVALUATION AND MOLECULAR DOCKING STUDY OF SOME 2(3-PYRIDYL)-THIAZOLYL-1,3,4-OXADIAZOLINES

CĂTĂLIN ARANICIU 1, OVIDIU ONIGA 2, GABRIEL MARC 2*, MARIANA DOINA PALAGE 1, LUMINIȚA MĂRUȚESCU 3,4, MARIANA CARMEN CHIFIRIUC 3,4, CRISTINA IOANA STOICA 1, IOANA IONUȚ 2, SMARANDA DAFINA ONIGA 1

1.“Iuliu Hațieganu” University of Medicine and Pharmacy, Faculty of Pharmacy, Department of Therapeutic Chemistry, 12 Ion Creangă Street, 400010, Cluj-Napoca, Romania
2.“Iuliu Hațieganu” University of Medicine and Pharmacy, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, 41 Victor Babeș Street, 400012, Cluj-Napoca, Romania
3.University of Bucharest, Faculty of Biology, Department of Microbiology, 1-3 Portocalelor Street, 60101, Bucharest, Romania
4.Research Institute of the University of Bucharest – ICUB, 91-95 Independenței Street, Bucharest, Romania

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Among the most promising unconventional targets for the development of new antimicrobial drugs is bacterial adherence and biofilm formation. This study is focused on the evaluation of a series of 2(3-pyridyl)-thiazolyl-1,3,4-oxadiazolines as bacterial biofilm inhibitors against a panel of Gram-positive bacterial strains. Some of these compounds showed interesting activity against biofilm formation of the Staphylococcus aureus strain. A preliminary study of the mechanism of action was carried out by a molecular docking assay between the compounds and the Sortase A enzyme. The connection between the docking results obtained and the anti-biofilm activity suggested that the tested compounds could have as potential mechanism of action the inhibition of Sortase A.