胸腺生成素Ⅱ活性肽片段——TP_5类似物的合成

SYNTHESIS OF THYMOPOIETIN Ⅱ ACTIVE FRAGMENT-TP_5 ANALOGS

为寻找高活性且耐酶水解的TP_5类免疫调节剂,根据TP_5的构效关系设计合成了一个三肽,二个五肽。肽链的合成采用DCC-HOBT和活化酯在液相中逐步偶联完成。将新型的碱敏α氨基保护基-Fmoc和新型精氨酸保护基-Mtr用于TP_5类似物的液相合成。肽中间体均经过元素分析鉴定,终产物经过质谱和氨基酸组分分析证实。

In order to search for TP_5-like immunomodulators with more potence and more resistance to enzymatic degradation, we designed and synthesized one tripeptide and two pentspeptides according to the structure-activity relationship of TP_5. The peptides were synthesized stepwise by DCC-HOBT and active ester methodes in liquid phase. The base-liableamino protective group 9-fluorenylmethyoxycarbenyl (Fmoc) and protective group for guanidine group of arginine—4-methyoxy-2, 3, 6-trimethybenzenesulfonyl [Mtr] were used in the synthesis of TP_5 analogs.The protected peptides were determined by elemental analysis. The tripeptide and pentspeptides were proved by mass spectrum and amino acid component analysis.