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Molecules 2017, 22(11), 1827;

New 2-Phenylthiazoles as Potential Sortase A Inhibitors: Synthesis, Biological Evaluation and Molecular Docking

Faculty of Pharmacy, “Iuliu Hațieganu” University of Medicine and Pharmacy, 8 Victor Babes St, 400012 Cluj-Napoca, Romania
Department of Microbiology, Faculty of Biology, University of Bucharest, 1-3 Portocalelor Street, 60101 Bucharest, Romania
Research Institute of the University of Bucharest-ICUB, 91-95 Independentei Street, 050095 Bucharest, Romania
National Institute for Research and Development of Isotopic and Molecular Technologies, 67-103 Donat Street, 400293 Cluj-Napoca, Romania
These authors contributed equally to this work.
Authors to whom correspondence should be addressed.
Received: 5 October 2017 / Accepted: 22 October 2017 / Published: 27 October 2017
(This article belongs to the Special Issue Focusing on Sulfur in Medicinal Chemistry)
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Sortase A inhibition is a well establish strategy for decreasing bacterial virulence by affecting numerous key processes that control biofilm formation, host cell entry, evasion and suppression of the immune response and acquisition of essential nutrients. A meta-analysis of structures known to act as Sortase A inhibitors provided the starting point for identifying a new potential scaffold. Based on this template a series of new potential Sortase A inhibitors, that contain the 2-phenylthiazole moiety, were synthesized. The physicochemical characterisation confirmed the identity of the proposed structures. Antibacterial activity evaluation showed that the new compounds have a reduced activity against bacterial cell viability. However, the compounds prevent biofilm formation at very low concentrations, especially in the case of E. faecalis. Molecular docking studies performed estimate that this is most likely due to the inhibition of Sortase A. The new compounds could be used as add-on therapies together with known antibacterial agents in order to combat multidrug-resistance enterococcal infections. View Full-Text
Keywords: 2-phenylthiazole; thiazole; antimicrobial; anti-biofilm activity; Sortase A inhibitor; enteroccocus 2-phenylthiazole; thiazole; antimicrobial; anti-biofilm activity; Sortase A inhibitor; enteroccocus

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Oniga, S.D.; Araniciu, C.; Palage, M.D.; Popa, M.; Chifiriuc, M.-C.; Marc, G.; Pirnau, A.; Stoica, C.I.; Lagoudis, I.; Dragoumis, T.; Oniga, O. New 2-Phenylthiazoles as Potential Sortase A Inhibitors: Synthesis, Biological Evaluation and Molecular Docking. Molecules 2017, 22, 1827.

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