氟化氨基膦酸钠盐的二肽类似物作为组织蛋白酶C的中度竞争性抑制剂。
Dipeptide analogues of fluorinated aminophosphonic acid sodium salts as moderate competitive inhibitors of cathepsin C.
作者信息
Wątroba Karolina, Pawełczak Małgorzata, Kaźmierczak Marcin
机构信息
Faculty of Chemistry, Adam Mickiewicz University in Poznań, Uniwersytetu Poznańskiego 8, 61-614 Poznań, Poland.
Institute of Chemistry, Opole University, 45-052 Opole, Poland.
出版信息
Beilstein J Org Chem. 2023 Apr 12;19:434-439. doi: 10.3762/bjoc.19.33. eCollection 2023.
In this paper, we present the solvolysis reaction of dipeptide analogues of fluorinated aminophosphonates with simultaneous quantitative deprotection of the amino group. To the best of our knowledge, this work is the first reported example of the application of fluorinated aminophosphonates in cathepsin C inhibition studies. The new molecules show moderate inhibition of the cathepsin C enzyme, which opens the door to consider them as potential therapeutic agents. Overall, our findings provide a new avenue for the development of fluorinated aminophosphonate-based inhibitors.
在本文中，我们展示了氟化氨基膦酸二肽类似物的溶剂解反应，同时对氨基进行定量脱保护。据我们所知，这项工作是氟化氨基膦酸在组织蛋白酶C抑制研究中应用的首个报道实例。新分子对组织蛋白酶C酶表现出适度的抑制作用，这为将它们视为潜在治疗剂打开了大门。总体而言，我们的研究结果为基于氟化氨基膦酸的抑制剂的开发提供了一条新途径。
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