Snyder Lawrence B, Meng Zhaoxing, Mate Robert, D'Andrea Stanley V, Marinier Anne, Quesnelle Claude A, Gill Patrice, DenBleyker Kenneth L, Fung-Tomc Joan C, Frosco MaryBeth, Martel Alain, Barrett John F, Bronson Joanne J
Bristol-Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, CT 06492, USA.
Bioorg Med Chem Lett. 2004 Sep 20;14(18):4735-9. doi: 10.1016/j.bmcl.2004.06.076.
A series of potential antimicrobial derivatives possessing bioisosteric replacements for the central oxazolidinone ring found in oxazolidinone antibacterials have been prepared. The design concept involved replacement of the requisite sp(3)-hybridized stereogenic center found at the 5-position of the oxazolidinone with a nitrogen atom. The synthesis and antibacterial activity of three such ring systems, the benzisoxazolinones, pyrroles, and isoxazolinones is described.
已制备了一系列具有生物电子等排体取代恶唑烷酮类抗菌药物中中心恶唑烷酮环的潜在抗菌衍生物。设计理念是用氮原子取代恶唑烷酮5位上必需的sp(3)杂化手性中心。描述了三种此类环系，即苯并异恶唑啉酮、吡咯和异恶唑啉酮的合成及抗菌活性。
