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Design at the atomic level: design of biaryloxazolidinones as potent orally active antibiotics
Authors:Zhou Jiacheng  Bhattacharjee Ashoke  Chen Shili  Chen Yi  Duffy Erin  Farmer Jay  Goldberg Joel  Hanselmann Roger  Ippolito Joseph A  Lou Rongliang  Orbin Alia  Oyelere Ayomi  Salvino Joe  Springer Dane  Tran Jennifer  Wang Deping  Wu Yusheng  Johnson Graham
Institution:Department of Medicinal Chemistry, Rib-X Pharmaceuticals Inc., 300 George Street, Suite 301, New Haven, CT 06511, USA.
Abstract:We have developed a first generation of hybrid sparsomycin-linezolid compounds into a new family of orally bioavailable biaryloxazolidinones that have activity against both linezolid-susceptible and -resistant gram-positive bacteria as well as the fastidious gram-negative bacteria Haemophilus influenzae and Moraxella catarrahalis. The convergent synthesis of these new compounds is detailed.
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