松属素及其衍生物的合成与抗菌活性  

Synthesis and antimicrobial activity of pinocembrin and its derivatives

作　　者：段亚波[1] 戚燕[1] 姬政[1] 方刚[1] 程永浩[1] 吴松[1] 

机构地区：[1]中国医学科学院中国协和医科大学药物研究所

出　　处：《中国药物化学杂志》2006年第6期342-346,共5页Chinese Journal of Medicinal Chemistry

摘　　要：目的合成松属素及其衍生物,研究其抗菌活性。方法以2,4,6-三羟基苯乙酮为起始原料,经羟基保护、缩合、环化、脱保护合成目标化合物。用平皿二倍稀释法研究目标化合物的体外抗菌活性。结果共得到18个目标化合物,经1H-NMR、MS确证其结构。初步药理实验结果表明,多数化合物表现出较好的体外抗菌活性。结论松属素及其衍生物有可能成为新型结构的抗菌药物。Aim To synthesize pinocembrin and its derivatives, and to study their antimicrobial activity. Methods Pinocembrin and its derivatives were synthesized with 2, 4, 6-trihydroxy-phenylethanone as the starting material via four steps including protection of the hydroxy-group, condensation, cyclization and deprotection.The in vitro antimicrobial activity was evaluated by the serial two-fold agar dilution method. Results Eighteen titled compounds were synthesized, their structure were confirmed by ^1H-NMR and MS analysis. The biological screening results demonstrated that most of the compounds prepared displayed potential antimicrobial activity. Conclusion Pinocembrin and its derivatives may be usefully antimicrobial candidate drugs.

关 键 词：药物化学 化合物制备 化学合成 黄烷酮 松属索 抗菌活性 

分 类 号：R914[医药卫生—药物化学]