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发明授权
US6147188A .alpha.- (1,3- or 1, 2- dicarbonylenol ether methyl ketones as cysteine protease inhibitors 失效
α-（1,3-或1,2-二羰基酚醚甲基酮作为半胱氨酸蛋白酶抑制剂）

.alpha.- (1,3- or 1, 2- dicarbonylenol ether methyl ketones as cysteine protease inhibitors
摘要：
Cysteine protease inhibitors which deactivate the protease by covalently bonding to the cysteine protease and releasing the enolate of a 1,3-dicarbonyl (or its enolic form). The cysteine protease inhibitors of the present invention accordingly comprise a first portion which targets a desired cysteine protease and positions the inhibitor near the thiolate anion portion of the active site of the protease, and a second portion which covalently bonds to the cysteine protease and irreversibly deactivates that protease by providing a carbonyl or carbonyl-equivalent which is attacked by the thiolate anion of the active site of the cysteine protease to sequentially cleave a .beta.-dicarbonyl enol ether leaving group.
摘要（中）：

半胱氨酸蛋白酶抑制剂，其通过共价键合到半胱氨酸蛋白酶并释放1,3-二羰基（或其烯醇形式）的烯醇化物而使蛋白酶失活。 因此，本发明的半胱氨酸蛋白酶抑制剂包含第一部分，其靶向所需的半胱氨酸蛋白酶，并将抑制剂置于蛋白酶活性位点的硫醇酸阴离子部分附近，第二部分与半胱氨酸蛋白酶共价结合并不可逆地失活 该蛋白酶通过提供被半胱氨酸蛋白酶的活性位点的硫醇盐阴离子攻击的羰基或羰基等价物来顺序地裂解β-二羰基烯醇醚离去基团。

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