高等学校化学学报Issue(11)：2362-2368,7.DOI:10.7503/cjcu20140223
马蹄金素杂环衍生物的合成及抗乙肝病毒活性
Synthesis and Anti-hepatitis B Virus Activities of Heterocyclic Substituted Matijin-Su Derivatives
摘要
Abstract
N-(N-Benzoyl-L-phenylalanyl)-O-acetyl-L-phenylalanol was isolated from Dichondra repens Forst. , which was a phenylalanine dipeptide compound with anti-HBV activity, named Matijin-Su( MTS) . Its chemi-cal skeleton structure was different from that of the existing drugs for anti-HBV. MTS was used as a lead com-pound base on the better anti-HBV activity by preliminary research. A series of MTS derivatives was designed and synthesized by a series of reactions, such as the formation of an amide( peptide) , hydrolysis, condensa-tion, acylation, alkylation and esterification using L-phenylalanine and its substitution as starting materials. The synthesized derivatives of MTS were characterized by 1 H NMR, 13 C NMR, ESI MS and elemental analysis. Their anti-hepatitis B virus activities against HepG2 2. 2. 15 cells line in vitro were tested. From the screening results, compounds 5b(IC50=8. 20 μg/L, SI=10. 26), 5g(IC50=5. 58 μg/L, SI=22. 78) and 5i (IC50=5. 07 μg/L, SI=16. 67) exhibited significant anti-HBV activities, the inhibition ratio were 56. 57%, 67. 06% and 66. 83%, respectively.关键词
马蹄金素/衍生物/杂环/抗乙肝病毒活性Key words
Matijin-Su/Derivative/Heterocyclic/Anti-HBV activity分类
化学化工引用本文复制引用
梁光平,胡占兴,刘青川,黄正明,张建新,梁光义,徐必学..马蹄金素杂环衍生物的合成及抗乙肝病毒活性[J].高等学校化学学报,2014,(11):2362-2368,7.基金项目
国家自然科学基金(批准号:81360472)和国家重大科学仪器设备开发专项(批准号:2011YQ12003506)资助 （批准号:81360472）
