1403670-15-4Relevant academic research and scientific papers
Elaboration of a proprietary thymidylate kinase inhibitor motif towards anti-tuberculosis agents
Song, Lijun,Risseeuw, Martijn D.P.,Froeyen, Matheus,Karalic, Izet,Goeman, Jan,Cappoen, Davie,Van der Eycken, Johan,Cos, Paul,Munier-Lehmann, Hélène,Van Calenbergh, Serge
, p. 5172 - 5182 (2016)
We report the design and synthesis of a series of non-nucleoside MtbTMPK inhibitors (1–14) based on the gram-positive bacterial TMPK inhibitor hit compound 1. A practical synthesis was developed to access these analogues. Several compounds show promising MtbTMPK inhibitory potency and allow the establishment of a structure–activity relationship, which is helpful for further optimization.
Discovery of selective and potent inhibitors of gram-positive bacterial thymidylate kinase (TMK)
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.
, p. 10010 - 10021 (2013/01/16)
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 sh
