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Structure-activity relationship in two series of aminoalkyl substituted coumarin inhibitors of gyrase B.
Authors:P Laurin  D Ferroud  L Schio  M Klich  C Dupuis-Hamelin  P Mauvais  P Lassaigne  A Bonnefoy  B Musicki
Affiliation:Medicinal Chemistry, Hoechst Marion Roussel, Romainville, France.
Abstract:Two series of aminosubstituted coumarins were synthesised and evaluated in vitro as inhibitors of DNA gyrase and as potential antibacterials. Novel novobiocin-like coumarins, 4-(dialkylamino)methylcoumarins and 4-((2-alkylamino)ethoxy)coumarins, were discovered as gyrase B inhibitors with promising antibacterial activity in vitro.
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