设计、合成及生物评价 L-多巴肽衍生物作为抗帕金森药物。
Design, synthesis and biological evaluation of peptide derivatives of L-dopa as anti-parkinsonian agents.
机构信息
School of Food Science and Biotechnology, Zhejiang Gongshang University, Hangzhou, Zhejiang 310035, PR China.
出版信息
Bioorg Med Chem Lett. 2013 Oct 1;23(19):5279-82. doi: 10.1016/j.bmcl.2013.08.007. Epub 2013 Aug 11.
A series of dipeptide derivatives of L-dopa were synthesized and investigated for their pharmacological activity using the unilaterally 6-hydroxydopamine (6-OHDA)-lesioned rat as an experimental model of Parkinson's disease. Among them, (S)-isopropyl 2-(2-amino-2-methylpropanamido)-3-(3,4-dihydroxyphenyl)propanoate (4 g) was found to be the most active compound, with 106% AUC activity and 149% peak activity of L-dopa after oral administration.
合成了一系列 L-多巴的二肽衍生物，并使用单侧 6-羟多巴胺（6-OHDA）损伤大鼠作为帕金森病的实验模型研究了它们的药理活性。其中，（S）-异丙基 2-（2-氨基-2-甲基丙酰胺基）-3-（3,4-二羟基苯基）丙氨酸酯（4 g）被发现是最活性化合物，口服后 L-多巴的 AUC 活性为 106%，峰值活性为 149%。
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