Zvarec, O.Polyak, S.Tieu, W.Kuan, K.Dai, H.Pedersen, D.Morona, R.Zhang, L.Booker, G.Abell, A.2012-09-062012-09-062012Bioorganic and Medicinal Chemistry Letters, 2012; 22(8):2720-27220960-894X1464-3405http://hdl.handle.net/2440/73039Herein 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.enCopyright © 2012 Elsevier Ltd. All rights reserved.Privileged scaffoldThiazolidinedioneRhodaninesAntibacterialStaphylococcus aureusJournal article002011832510.1016/j.bmcl.2012.02.1000003027682000142-s2.0-8486280721524909Polyak, S. [0000-0002-8458-5194]Tieu, W. [0000-0002-7161-4152]Morona, R. [0000-0001-7009-7440]Booker, G. [0000-0001-7207-4699]Abell, A. [0000-0002-0604-2629]