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5-benzylidenerhodanine and 5-benzylidene-2-4-thiazolidinedione based antibacterials.

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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Zvarec O,Polyak SW,Tieu W,Kuan K,Dai H,Pedersen DS,Morona R,Zhang L,Booker GW,Abell AD

doi

10.1016/j.bmcl.2012.02.100

subject

Has Abstract

pub_date

2012-04-15 00:00:00

pages

2720-2

issue

8

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(12)00302-2

journal_volume

22

pub_type

杂志文章

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