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Improved antibacterial activities of coumarin antibiotics bearing 5',5'-dialkylnoviose: biological activity of RU79115
Authors:Musicki B  Periers A M  Laurin P  Ferroud D  Benedetti Y  Lachaud S  Chatreaux F  Haesslein J L  Iltis A  Pierre C  Khider J  Tessot N  Airault M  Demassey J  Dupuis-Hamelin C  Lassaigne P  Bonnefoy A  Vicat P  Klich M
Institution:Medicinal Chemistry, Hoechst Marion Roussel/Aventis, Romainville, France. branislav.musicki@aventis.com
Abstract:A new series of coumarin inhibitors of DNA gyrase B bearing a N-propargyloxycarbamate at C-3' of various 5',5'-dialkylnoviose, including RU79115, were synthesised and their antibacterial activities have been delineated. Introduction of dialkyl substituents at 5'5'-position of noviose leads to coumarin analogues with improved in vitro and in vivo antibacterial activity.
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