多肽化合物AcSDKP衍生物的设计与合成  

Design and synthesis of AcSDKP related peptides

作　　者：倪成[1] 朱辉[2] 邓桂茹[2] 韩香[2] NI Cheng;ZHU Hui;DENG Gui-ru;HAN Xiang(Postgraduate Team 1,Logistics University of PAP,Tianjin 300309,China)

机构地区：[1]武警后勤学院研究生大队一队,天津300309 [2]武警后勤学院基础部,天津300309

出　　处：《武警后勤学院学报（医学版）》2018年第3期185-189,共5页Journal of Logistics University of PAP（Medical Sciences）

基　　金：国家自然科学基金项目(21142011);天津市自然科学基金项目(13JCYBJC24700)

摘　　要：【目的】以AcSDKP为先导结构,设计并合成具有化学损伤防护活性的多肽化合物。【方法】采用固相多肽合成或液相方法获得目标产物,涉及的结构改造方式主要有C末端的修饰、N末端的修饰、侧链修饰与残基的位点改造等。【结果】17个目的产物结构经LC-MS分析证明,相对分子质量与理论值一致;粗产物经RP-HPLC分离分析,纯度达到95%以上。【结论】通过本设计与合成工作,为开发具有化学损伤保护活性的新药提供实验依据。【Objective】To design and synthesize the polypeptide compounds with chemical damage protection activity in a lead structure of Ac SDKP. 【Methods】 Target products were prepared by solid phase peptide synthesis or liquid phase method. The structural transformation modes included substitution or modification of N-, C-terminus, or side chains with unnatural building blocks as the surrogates for normal residues.【Results】The structures of 17 target products were confirmed by LC-MS analysis that the relative molecular weight was consistent with the theoretical value, and the purity of the crude product was over 95% by RP-HPLC separation and analysis.【Conclusion】By the design and synthesis, the experimental basis is provided for the development of new drugs with chemical damage protection activity.

关 键 词：ACSDKP 化学损伤防护 结构改造 

分 类 号：R914.2[医药卫生—药物化学]