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New antibacterial tetrahydro-4(2H)-thiopyran and thiomorpholine S-oxide and S,S-dioxide phenyloxazolidinones |
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| Authors: | Singh Upinder Raju B Lam Stuart Zhou Joseph Gadwood Robert C Ford Charles W Zurenko Gary E Schaadt Ronda D Morin Sara E Adams Wade J Friis Janice M Courtney Maria Palandra Joe Hackbarth Corinne J Lopez Sara Wu Charlotte Mortell Kathleen H Trias Joaquim Yuan Zhengyu Patel Dinesh V Gordeev Mikhail F |
| Affiliation: | Vicuron Pharmaceuticals Inc., 34790 Ardentech Court, Fremont, CA 94555, USA. |
| Abstract: | Combinatorial libraries of N-acylated 5-(S)-aminomethyloxazolidinone derivatives of S-oxide and S,S-dioxide tetrahydro-4(2H)-thiopyranyl and thiomorpholine phenyloxazolidinone series have been synthesized on a solid phase and evaluated for antimicrobial activity. Several novel potent leads have been identified, including orally active oxazolidinones with enhanced activity against respiratory tract infection pathogens Haemophilus influenzae and Moraxella catarrhalis. |
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