Author/Authors :
Patrick Laurin، نويسنده , , Didier Ferroud، نويسنده , , Michel Klich، نويسنده , , Claudine Dupuis-Hamelin، نويسنده , , Pascale Mauvais، نويسنده , , Patrice Lassaigne، نويسنده , , Alain Bonnefoy، نويسنده , , Branislav Musicki، نويسنده ,
Abstract :
The design, synthesis, and in vitro biological activity of a series of novel coumarin inhibitors of gyrase B is presented. Replacement of the 3-acylamino residue (3-NHCOR) of coumarin drugs with reversed isosteres C(=O)R, C(=N-OR)Rʹ, COOR, CONHR and CONHOR leads to highly potent analogues which displayed excellent inhibition of the negative supercoiling of the relaxed DNA and antibacterial activity.
