Design and solid phase synthesis of the 1,3,4-oxadiazole based peptidomimetic library is presented. Library synthesis starts from the coupling of the thiosemicarbazide resin with Fmoc-protected amino acid following desulfurative cyclization to 1,3,4-oxadiazoles. Following substitution of the secondary amine with the 3-nitrobenzoyl functional group and its further reduction were performed. Thus, the functionalization with amino acids could be performed on both sides of the core skeleton. After diversification and cleavage from the resin using TFA: DCM cleavage cocktail, an enantiopure library of compounds was obtained. Further evaluation of physicochemical properties was performed.

介绍了基于1,3,4-恶二唑的拟肽文库的设计和固相合成。文库的合成开始于将硫代氨基脲树脂与Fmoc保护的氨基酸偶联，然后脱硫环化成1,3,4-恶二唑。用3-硝基苯甲酰基官能团取代仲胺后，将其进一步还原。因此，可以在核心骨架的两侧进行氨基酸官能化。使用TFA：DCM裂解混合物从树脂中裂解并裂解后，获得了对映体纯的化合物文库。进行了进一步的理化性质评估。