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https://hdl.handle.net/2440/73039
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Type: | Journal article |
Title: | 5-Benzylidenerhodanine and 5-benzylidene-2-4-thiazolidinedione based antibacterials |
Author: | Zvarec, O. Polyak, S. Tieu, W. Kuan, K. Dai, H. Pedersen, D. Morona, R. Zhang, L. Booker, G. Abell, A. |
Citation: | Bioorganic and Medicinal Chemistry Letters, 2012; 22(8):2720-2722 |
Publisher: | Pergamon-Elsevier Science Ltd |
Issue Date: | 2012 |
ISSN: | 0960-894X 1464-3405 |
Statement of Responsibility: | Ondrej Zvarec, Steven W. Polyak, William Tieu, Kevin Kuan, Huanqin Dai, Daniel Sejer Pedersen, Renato Morona, Lixin Zhang, Grant W. Booker, Andrew D. Abell |
Abstract: | Herein we outline the antibacterial activity of amino acid containing thiazolidinediones and rhodanines against Gram-positive bacteria Staphylococcus aureus ATCC 31890, Staphylococcus epidermidis and Bacillus subtilis ATCC 6633. The rhodanine derivatives were generally more active than the analogous thiazolidinediones. Compounds of series 5 showed some selectivity for Bacillus subtilis ATCC 6633, the extent of which is enhanced by the inclusion of a non-polar amino acid at the 5-position of the core thiazolidinediones and rhodanines scaffolds. SAR data of series 8 demonstrated improved activity against the clinically more significant Staphylococci with selectivity over Bacillus subtilis ATCC 6633 induced by introduction of a bulky aryl substituent at the 5-position of the core scaffolds. |
Keywords: | Privileged scaffold Thiazolidinedione Rhodanines Antibacterial Staphylococcus aureus |
Rights: | Copyright © 2012 Elsevier Ltd. All rights reserved. |
DOI: | 10.1016/j.bmcl.2012.02.100 |
Grant ID: | ARC |
Published version: | http://dx.doi.org/10.1016/j.bmcl.2012.02.100 |
Appears in Collections: | Aurora harvest IPAS publications Molecular and Biomedical Science publications |
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