1,5-Regioisomeric triazole linked disaccharides have been synthesized and screened for their inhibitory properties against ribonuclease A (RNase A). The angular constraint-driven ‘crescent shaped’ inhibitors accommodated themselves into the enzyme active site. An improved enzyme inhibition was observed with increased H-bonding ability of polar functional groups in the modified disaccharides. In this series, introduction of two carboxyl groups in the furanose rings elicited the best result with an inhibition constant of 50 ± 3 µM. This is the first ever report on the use of disaccharides as RNase A inhibitors.

中文翻译：

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1,5-二取代的1,2,3-三唑连接的二糖：无金属合成和新型核糖核酸酶A抑制剂的筛选

已经合成了1，5-区域异构的三唑连接的二糖，并筛选了它们对核糖核酸酶A（RNase A）的抑制特性。角度约束驱动的“新月形”抑制剂使其自身进入酶活性位点。在修饰的二糖中观察到改善的酶抑制作用以及极性官能团的H键结合能力增强。在该系列中，在呋喃糖环中引入两个羧基可产生最佳结果，其抑制常数为50±3 µM。这是关于使用二糖作为RNase A抑制剂的首次报道。