Next Article in Journal
Design of Tail-Clamp Peptide Nucleic Acid Tethered with Azobenzene Linker for Sequence-Specific Detection of Homopurine DNA
Next Article in Special Issue
Syntheses of Novel 4-Substituted N-(5-amino-1H-1,2,4-triazol-3-yl)pyridine-3-sulfonamide Derivatives with Potential Antifungal Activity
Previous Article in Journal
Identification for the First Time of Cyclo(d-Pro-l-Leu) Produced by Bacillus amyloliquefaciens Y1 as a Nematocide for Control of Meloidogyne incognita
Previous Article in Special Issue
Evaluation of LPS-Induced Acute Lung Injury Attenuation in Rats by Aminothiazole-Paeonol Derivatives
Article Menu

Export Article

Open AccessArticle
Molecules 2017, 22(11), 1827; doi:10.3390/molecules22111827

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

1
Faculty of Pharmacy, “Iuliu Hațieganu” University of Medicine and Pharmacy, 8 Victor Babes St, 400012 Cluj-Napoca, Romania
2
Department of Microbiology, Faculty of Biology, University of Bucharest, 1-3 Portocalelor Street, 60101 Bucharest, Romania
3
Research Institute of the University of Bucharest-ICUB, 91-95 Independentei Street, 050095 Bucharest, Romania
4
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)
View Full-Text   |   Download PDF [3319 KB, uploaded 1 November 2017]   |  

Abstract

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
Figures

Figure 1

This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

Scifeed alert for new publications

Never miss any articles matching your research from any publisher
  • Get alerts for new papers matching your research
  • Find out the new papers from selected authors
  • Updated daily for 49'000+ journals and 6000+ publishers
  • Define your Scifeed now

SciFeed Share & Cite This Article

MDPI and ACS Style

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.

Show more citation formats Show less citations formats

Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Related Articles

Article Metrics

Article Access Statistics

1

Comments

[Return to top]

Molecules EISSN 1420-3049 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert
Back to Top