双噁唑烷酮类化合物的合成及体外抗菌活性

芳基二胺与（R）-正丁酸缩水甘油酯缩合得（R，R）-1，4-双-（2-羟基-3-丁酰氧基）-丙氨基]-芳烃（3a和3b），与羰基二咪唑环合构成双噁唑烷酮4a和4b，水解脱丁酰基得（R，R）-1，4-双-（5-羟甲基-2-氧代噁唑烷-3-基）-芳烃（5a和5b）、再经甲磺酰化、叠氮化、还原叠氮基所得产物氨基乙酰化得（S，S）-1，4-双-（5-乙酰氨甲基-2-氧代噁唑烷-3-基）-芳烃（8a和8b），结构经^1HNMR和MS确证，并进行体外抗菌活性试验。结果表明，化合物5b对表葡菌，肠球菌和丙型链球菌的活性优于吗啉噁酮。

Synthesis and in vitro Antibacterial Activities of Some Bis-Oxazolidinones

Aryl diamines were condensed with (R)-glycidyl butyrate to form (R,R)-l,4-bis-(2-hydroxyl-3-butyryloxy)-propylamino] benzene derivatives (3a and 3b), which were cyclized with carbonyldiimidazole to get the bis-oxazolidinones(4a and 4b), the latter were hydrolyzed into (R,R)-l,4-bis-(5-hydroxymethyl-2-oxo-oxazolidin-3-yl)benzene derivatives (5a and 5b). Compounds 5a and 5b were converted via 6a, 6b and 7a, 76 to (S,S)-1,4-bis-(5-acetamidomethyl-2-oxo-oxazolidinyl-3)benzene derivatives (8a and 8b). The structures of these new compounds were confirmed by HNMR and MS. The in vitro antibacterial activities on 20 bacteria were tested and the result showed that compd 5b had better activity than linezolid against Staphylococcus epidermidis, Staphylococcus enteridis and Staphylococcus nonhemolyticus.