1403881-74-2Relevant articles and documents
Design, synthesis and structure-activity relationships of substituted oxazole-benzamide antibacterial inhibitors of FtsZ
Stokes, Neil R.,Baker, Nicola,Bennett, James M.,Chauhan, Pramod K.,Collins, Ian,Davies, David T.,Gavade, Maruti,Kumar, Dushyant,Lancett, Paul,Macdonald, Rebecca,MaCleod, Leanne,Mahajan, Anu,Mitchell, Jeffrey P.,Nayal, Narendra,Nayal, Yashodanand Nandan,Pitt, Gary R.W.,Singh, Mahipal,Yadav, Anju,Srivastava, Anil,Czaplewski, Lloyd G.,Haydon, David J.
, p. 353 - 359 (2015/09/08)
The design, synthesis and structure-activity relationships of a series of oxazole-benzamide inhibitors of the essential bacterial cell division protein FtsZ are described. Compounds had potent anti-staphylococcal activity and inhibited the cytokinesis of the clinically-significant bacterial pathogen Staphylococcus aureus. Selected analogues possessing a 5-halo oxazole also inhibited a strain of S. aureus harbouring the glycine-to-alanine amino acid substitution at residue 196 of FtsZ which conferred resistance to previously reported inhibitors in the series. Substitutions to the pseudo-benzylic carbon of the scaffold improved the pharmacokinetic properties by increasing metabolic stability and provided a mechanism for creating pro-drugs. Combining multiple substitutions based on the findings reported in this study has provided small-molecule inhibitors of FtsZ with enhanced in vitro and in vivo antibacterial efficacy.
AROMATIC AMIDES AND USES THEREOF
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Page/Page column 99, (2012/11/07)
The present invention provides compounds of Formula (I): and salts, racemates, isomers, diastereoisomers, enantiomers, hydrates, solvates, N-oxides, pharmaceutically acceptable derivatives or prodrugs thereof. Also provided the use of these compounds as antibacterials, compositions comprising them and processes for their manufacture.
