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Martínez-Botella, Gabriel; Breen, John N; Duffy, James E. S; Dumas, Jacques; Geng, Bolin; Gowers, Ian K; Green, Oluyinka M; Guler, Satenig; Hentemann, Martin F; Hernandez-Juan, Felix A; Joseph-McCarthy, Diane; Kawatkar, Sameer; Larsen, Nicholas A; Lazari, Ovadia; Loch, James T; Macritchie, Jacqueline A; McKenzie, Andrew R; Newman, Joseph V; Olivier, Nelson B; Otterson, Linda G; Owens, Andrew P; Read, Jon; Sheppard, David W; Keating, Thomas A
Journal of medicinal chemistry, 11/2012, Letnik: 55, Številka: 22Journal Article
Thymidylate kinase (TMK) is an essential enzyme in bacterial DNA synthesis. The deoxythymidine monophosphate (dTMP) substrate binding pocket was targeted in a rational-design, structure-supported effort, yielding a unique series of antibacterial agents showing a novel, induced-fit binding mode. Lead optimization, aided by X-ray crystallography, led to picomolar inhibitors of both Streptococcus pneumoniae and Staphylococcus aureus TMK. MICs < 1 μg/mL were achieved against methicillin-resistant S. aureus (MRSA), S. pneumoniae, and vancomycin-resistant Enterococcus (VRE). Log D adjustments yielded single diastereomers 14 (TK-666) and 46, showing a broad antibacterial spectrum against Gram-positive bacteria and excellent selectivity against the human thymidylate kinase ortholog.
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JCR | SNIP | JCR | SNIP | JCR | SNIP | JCR | SNIP |
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in: SICRIS
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