CAJ | 학술논문

以马蹄金素[ N-( N-苯甲酰基-L-苯丙氨酰基)-O-乙酰基-L-苯丙氨醇, MTS]为先导化合物,设计并合成了16个杂环取代的马蹄金素衍生物,其结构经NMR, ESI-MS和元素分析确证.以HepG22.2.15细胞为乙肝病毒( HBV)载体,对合成的马蹄金素衍生物进行了抗HBV活性测试.实验结果表明,在测试浓度范围内,化合物5b(IC50=8.20μg/L, SI=10.26),5g(IC50=5.58μg/L, SI=22.78)和5i(IC50=5.07μg/L, SI=16.67)的抗HBV活性较强；在8μg/mL的浓度下,其抑制率分别为56.57%,67.06%和66.83%.
이마제금소[ N-( N-분갑선기-L-분병안선기)-O-을선기-L-분병안순, MTS]위선도화합물,설계병합성료16개잡배취대적마제금소연생물,기결구경NMR, ESI-MS화원소분석학증.이HepG22.2.15세포위을간병독( HBV)재체,대합성적마제금소연생물진행료항HBV활성측시.실험결과표명,재측시농도범위내,화합물5b(IC50=8.20μg/L, SI=10.26),5g(IC50=5.58μg/L, SI=22.78)화5i(IC50=5.07μg/L, SI=16.67)적항HBV활성교강；재8μg/mL적농도하,기억제솔분별위56.57%,67.06%화66.83%.
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.