前药
化学
寡肽
布洛芬
结合
萘普生
谷氨酸
药理学
药物输送
部分
靶向给药
药品
肽
组合化学
生物化学
氨基酸
立体化学
医学
有机化学
替代医学
病理
数学分析
数学
作者
Yi Zhao,Dongsheng He,Lifang Ma,Li Guo
出处
期刊:Letters in Drug Design & Discovery
[Bentham Science]
日期:2015-06-06
卷期号:12 (7): 585-590
被引量:11
标识
DOI:10.2174/1570180812999150217171229
摘要
Osteoarthritis is no doubt a difficult disease to manage. Targeted delivery of drugs to bone may not only enhance the treatment efficacy, but also reduces the quantity of drug administered. In this paper, we have synthesized two series of NSAID-Glu oligopeptide conjugates built up by the therapeutic moiety (naproxen and ibuprofen) and the targeting moieties (Glutamic oligopeptides) via amide linkage, as novel potential bone-targeting NSAIDs prodrugs. Preliminary studies indicated that these prodrugs exhibited outstanding hydroxyapatite affinity, furthermore, NSAIDs-glutamic hexa-peptide conjugates were found more potent in hydroxyapatite binding. The adequate chemical stability of the conjugates in different buffers, indicated that the conjugates might become a promising approach of selective delivery of drugs to bone tissues. These results may be conducive to the study of bone targeting drugs delivery. Keywords: Synthesis, bone-targeting, prodrug, NSAID, glutamic acid oligopeptide, Hydroxyapatite affinity.
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