229307-63-5Relevant academic research and scientific papers
Coumarin inhibitors of gyrase B with N-propargyloxy-carbamate as an effective pyrrole bioisostere
Periers, Anne-Marie,Laurin, Patrick,Ferroud, Didier,Haesslein, Jean-Luc,Klich, Michel,Dupuis-Hamelin, Claudine,Mauvais, Pascale,Lassaigne, Patrice,Bonnefoy, Alain,Musicki, Branislav
, p. 161 - 165 (2007/10/03)
The synthesis and biological profile in vitro of a series of coumarin inhibitors of gyrase B bearing a N-propargyloxycarbamate at C-3' of noviose is presented. Replacement of the 5-methylpyrrole-2-carboxylate of coumarin drugs with an N-propargyloxycarbamate bioisostere leads to analogues with improved antibacterial activity. Analysis of crystal structures of coumarin antibiotics with the 24 kDa N-terminal domain of the gyrase B protein provides a rational for the excellent inhibitory potency of C-3' N- alkoxycarbamates.
