New antibacterial tetrahydro-4(2H)-thiopyran and thiomorpholine S-oxide and S,S-dioxide phenyloxazolidinones.
Singh U, Raju B, Lam S, Zhou J, Gadwood RC, Ford CW, Zurenko GE, Schaadt RD, Morin SE, Adams WJ, Friis JM, Courtney M, Palandra J, Hackbarth CJ, Lopez S, Wu C, Mortell KH, Trias J, Yuan Z, Patel DV, Gordeev MF.
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.