Department of Medicinal Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, PR China.
Bioorg Med Chem Lett. 2011 Nov 15;21(22):6674-7. doi: 10.1016/j.bmcl.2011.09.060. Epub 2011 Sep 21.
A series of new substituted 4-amino-N-(diaminomethylene) benzenesulfonamides were synthesized and their in vitro acrosin inhibitory activities were evaluated. Most of the compounds showed potent acrosin inhibitory activities with compounds 4o and 4p being significantly more potent than the control compound N-alpha-tosyl-L-lysyl-chloromethyl-ketone (TLCK). The compounds provide a new scaffold for the development of acrosin inhibitory agents.
一系列新的取代的 4-氨基-N-(二氨基亚甲基)苯磺酰胺被合成，并评估了它们的体外顶体蛋白酶抑制活性。大多数化合物表现出很强的顶体蛋白酶抑制活性，其中化合物 4o 和 4p 比对照化合物 N-α-对甲苯磺酰基-L-赖氨酰-氯甲基-酮（TLCK）的活性显著增强。这些化合物为开发顶体蛋白酶抑制剂提供了一个新的结构骨架。
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