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近年来,在天然或非天然生物活性化合物的合成杂合体的药物化学发展方面取得了进展。

Recent progress in the development of synthetic hybrids of natural or unnatural bioactive compounds for medicinal chemistry.

机构信息

Department of Chemistry and Pharmacy, University of Erlangen-Nuremberg, Erlangen, Germany.

出版信息

Mini Rev Med Chem. 2010 Aug;10(9):773-93. doi: 10.2174/138955710791608280.

DOI:10.2174/138955710791608280
PMID:20105118
Abstract

The present mini-review highlights the recent developments on different classes of synthetic hybrids of natural and/or unnatural bioactive compounds, the utilization of which is very promising, as distinct features of each component can be hybridized and their properties leveraged. Particular stress is put on the respective mode of action and the corresponding rationale behind covalent combinations of various bioactive agents to increase their therapeutic potential, facilitate their administration, to reduce harmful side effects and/or to overcome the problem of multi-drug resistance. This rather recent approach has already found applications in the development of new anti-cancer, anti-Alzheimer, anti-malaria, anti-microbial therapeutics and other novel compounds with unprecedented bioactivity.

摘要

本篇小型综述强调了天然和/或非天然生物活性化合物的不同类别合成杂合体的最新进展,由于每个成分的独特特征可以杂交并利用其性质,因此它们的应用非常有前景。特别强调了各种生物活性药物的共价结合背后的各自作用模式和相应原理,以提高其治疗潜力,使其更容易给药,减少有害的副作用和/或克服多药耐药性问题。这种相对较新的方法已经在开发新的抗癌、抗老年痴呆症、抗疟疾、抗微生物疗法和其他具有前所未有的生物活性的新型化合物中得到了应用。

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