New antibacterial tetrahydro-4(2H)-thiopyran and thiomorpholine S-oxide and S,S-dioxide phenyloxazolidinones.

作者信息

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

机构信息

Vicuron Pharmaceuticals Inc., 34790 Ardentech Court, Fremont, CA 94555, USA.

出版信息

Bioorg Med Chem Lett. 2003 Dec 1;13(23):4209-12. doi: 10.1016/j.bmcl.2003.07.022.

DOI:10.1016/j.bmcl.2003.07.022

PMID:14623003

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.

摘要