Peptides conjugated with organic molecules can be useful tools for the development of novel bioactive compounds. The lysine side‐chain is an interesting functional group to act as a linker to connect small molecules in peptide conjugates. Herein we present the design and synthesis of four Safirinium derivatives, their facile conjugation to lysine in solid phase, and incorporation in peptides. The compounds differing in the functionalization of nitrogen N2 of the condensed triazolyl moiety are novel building blocks to design conjugates to perform structure‐activity relationship studies of elastase inhibitors. Consequently, structural investigations of the lysine building blocks and of the corresponding peptide conjugates were performed. We present herein the potential of the Safirinium analogs to act as elastase inhibitors in assays performed on porcine pancreas elastase

中文翻译：

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用三唑衍生物制备生物活性赖氨酸和肽缀合物的合成策略


与有机分子缀合的肽可以成为开发新型生物活性化合物的有用工具。赖氨酸侧链是一个有趣的官能团，可作为连接肽缀合物中小分子的接头。在此，我们介绍了四种 Safirinium 衍生物的设计和合成、它们在固相中与赖氨酸的轻松缀合以及在肽中的掺入。缩合三唑基部分的氮 N2 官能化不同的化合物是设计缀合物以进行弹性蛋白酶抑制剂构效关系研究的新型构建模块。因此，对赖氨酸结构单元和相应的肽缀合物进行了结构研究。我们在此介绍了 Safirinium 类似物在猪胰腺弹性蛋白酶测定中作为弹性蛋白酶抑制剂的潜力