Author/Authors :
Jiacheng Zhou، نويسنده , , Ashoke Bhattacharjee، نويسنده , , Shili Chen، نويسنده , , Yi Chen، نويسنده , , Erin Duffy، نويسنده , , Jay Farmer، نويسنده , , Joel Goldberg، نويسنده , , Roger Hanselmann، نويسنده , , Joseph A. Ippolito، نويسنده , , Rongliang Lou، نويسنده , , Alia Orbin، نويسنده , , Ayomi Oyelere، نويسنده , , Joe Salvino، نويسنده , , Dane Springer، نويسنده , , Jennifer Tran، نويسنده , , Chengjie Zhao and Deping Wang، نويسنده , , Yusheng Wu، نويسنده , , Graham Johnson، نويسنده ,
Abstract :
From the X-ray crystal structures of linezolid and the non-selective antibiotic sparsomycin, we have derived a new family of hybrid oxazolidinones. From this initial compound set we have developed a new biaryloxazolidinone scaffold that shows both potent antimicrobial activity as well as selective inhibition of ribosomal translation. The synthesis of these compounds is outlined.
Keywords :
Linezolid , Sparsomycin , Gram-negative bacteria , X-ray crystal structure , Oral antibiotics , ribosome , Hybrid antibiotics , Oxazolidinone , structure-based drug design , Biaryloxazolidinone