西罗莫司结构修饰的研究进展

Structural modifications of sirolimus:research advances

自西罗莫司作为免疫抑制剂应用于临床以来,便受到了人们的广泛关注。随着研究的深入,其生物利用度低、疏水性差以及结构不稳定等缺点的存在,使得该抗生素的临床应用受到了一定的限制,因此开发新型西罗莫司衍生物具有重要的研究和应用价值。近年人们对西罗莫司进行了大量的结构修饰研究,并从中获得了一系列有价值的衍生物。本文对西罗莫司结构修饰的最新研究进展作了一个简要的综述,并重点对几个结构修饰成功的西罗莫司衍生物作了较为详细的介绍。

Sirolimus was paid extensive attention since it was applied as immunosuppressant in clinic. Along with further study, the drawbacks of sirolimus such as the low bioavailability, low hydrophobic property and the instability of its structure restrict the clinic applications, therefore, it is necessary to explore new sirolimus derivatives. In the recent years, lots of study on the structural modifications of sirolimus have been made and obtained a series of valuable derivatives. This paper summarizes the structural modificatory advance of sirolimus and mainly introduces several successful sirolimus derivatives.