Phosphinate, sulfonate, and sulfonamidate dipeptides as potential inhibitors of Escherichia coli aminopeptidase N.
Phosphinate, sulfonate, and sulfonamidate dipeptides as potential inhibitors of Escherichia coli aminopeptidase N.
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DOI：
10.1016/j.bmcl.2005.08.055
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发表时间：
2005-12
影响因子：
2.7
通讯作者：
Ke-Wu Yang;Frank C Golich;T. Sigdel;M. Crowder
中科院分区：
文献类型：
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作者：
Ke-Wu Yang;Frank C Golich;T. Sigdel;M. Crowder
为了制备新型的细菌氨肽酶N（PepN）抑制剂，合成了Ala-Ala的次膦酸酯、丙烯基次膦酸酯、癸基次膦酸酯、磺酸酯和磺酰胺酯类似物，并作为抑制剂进行了测试。亚膦酸酯1显示出抑制PepN，Ki为10μM，丙烯基亚膦酸酯2和癸基亚膦酸酯3抑制PepN，Ki为约10 μ M。1μM。磺酸盐和磺酰胺盐类似物不抑制PepN。
In an effort to prepare novel inhibitors of bacterial aminopeptidase N (PepN), the phosphinate, propenylphosphinate, decylphosphinate, sulfonate, and sulfonamidate analogs of Ala–Ala were synthesized and tested as inhibitors. Phosphinate 1 was shown to inhibit PepN with a Kiof 10μM, and propenylphosphinate 2 and decylphosphinate 3 inhibited PepN with a Kiof ca. 1μM. Sulfonate and sulfonamidate analogs did not inhibit PepN.