5-Benzylidenerhodanine and 5-benzylidene-2-4-thiazolidinedione based antibacterials

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dc.contributor.authorZvarec, O.
dc.contributor.authorPolyak, S.
dc.contributor.authorTieu, W.
dc.contributor.authorKuan, K.
dc.contributor.authorDai, H.
dc.contributor.authorPedersen, D.
dc.contributor.authorMorona, R.
dc.contributor.authorZhang, L.
dc.contributor.authorBooker, G.
dc.contributor.authorAbell, A.
dc.date.issued2012
dc.description.abstractHerein 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.
dc.description.statementofresponsibilityOndrej Zvarec, Steven W. Polyak, William Tieu, Kevin Kuan, Huanqin Dai, Daniel Sejer Pedersen, Renato Morona, Lixin Zhang, Grant W. Booker, Andrew D. Abell
dc.identifier.citationBioorganic and Medicinal Chemistry Letters, 2012; 22(8):2720-2722
dc.identifier.doi10.1016/j.bmcl.2012.02.100
dc.identifier.issn0960-894X
dc.identifier.issn1464-3405
dc.identifier.orcidPolyak, S. [0000-0002-8458-5194]
dc.identifier.orcidTieu, W. [0000-0002-7161-4152]
dc.identifier.orcidMorona, R. [0000-0001-7009-7440]
dc.identifier.orcidBooker, G. [0000-0001-7207-4699]
dc.identifier.orcidAbell, A. [0000-0002-0604-2629]
dc.identifier.urihttp://hdl.handle.net/2440/73039
dc.language.isoen
dc.publisherPergamon-Elsevier Science Ltd
dc.relation.grantARC
dc.rightsCopyright © 2012 Elsevier Ltd. All rights reserved.
dc.source.urihttps://doi.org/10.1016/j.bmcl.2012.02.100
dc.subjectPrivileged scaffold
dc.subjectThiazolidinedione
dc.subjectRhodanines
dc.subjectAntibacterial
dc.subjectStaphylococcus aureus
dc.title5-Benzylidenerhodanine and 5-benzylidene-2-4-thiazolidinedione based antibacterials
dc.typeJournal article
pubs.publication-statusPublished

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