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  • Title: 5-benzylidenerhodanine and 5-benzylidene-2-4-thiazolidinedione based antibacterials.
    Author: Zvarec O, Polyak SW, Tieu W, Kuan K, Dai H, Pedersen DS, Morona R, Zhang L, Booker GW, Abell AD.
    Journal: Bioorg Med Chem Lett; 2012 Apr 15; 22(8):2720-2. PubMed ID: 22444680.
    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.
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