新型恶唑烷酮化合物对耐药性结核 分枝杆菌抗菌作用的探讨

Efficacy of novel Oxazolidinone analogues against MDR mycobacterial tuberculosis

摘要:

目的 测定新型恶唑烷酮化合物对临床分离的广泛耐药结核分枝杆菌的抗菌活性。方法 采用 7H10 培养基进行体外菌落培养及最小抑菌浓度测定。采用BALB/c 小鼠攻毒结核分枝杆菌模型测定化合物 的抗菌活性。结果 新型恶唑烷酮化合物sy142 在体外检测和动物模型中的抗结核活性均优于linezolid，sy144 与linezolid 活性相当。Sy142 与sy144 对多重耐药结核分枝杆菌和广泛耐药结核分枝杆菌具有强效的抗菌作用。 结论 sy142 和sy144 抗结核活性强，可作为新型恶唑烷酮抗菌剂研发的先导化合物。

Abstract:

Objective To test the efficacy of novel Oxazolidinone analogues against multi-drug resistant (MDR) mycobacterial tuberculosis. Methods Tube dilution method and Middlebrook 7H10 agar media were utilized to determine the anti-bacterial activities of Oxazolidinones analogues. In vivo activities of these compounds were evaluated with BALB/c mouse model of mycobacterial tuberculosis infection. Results Sy142 indicated improved anti-bacterial efficacyboth in vitro and in vivo when compared with Linezolid, and sy144 manifested similar activities compared with Linezolid. Both sy142 and sy144 demonstrated promising efficacy of anti-bacterial activities against MDR Mycobacterial tuberculosis. Conclusions Sy142 and sy144 exerts satisfactory anti-MDR mycobacterial tuberculosisefficacy and is acceptable for further structural modifications.