title: Synthesis and acrosin inhibitory activity of substituted 4-amino-N-(diaminomethylene) benzenesulfonamide derivatives.
abstract: 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.
authors: Department of Medicinal Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, PR China.
authors: Lili
authors: L
authors: Ding
authors: Ju
authors: J
authors: Zhu
authors: Canhui
authors: C
authors: Zheng
authors: Chunquan
authors: C
authors: Sheng
authors: Jingjing
authors: J
authors: Qi
authors: Xuefei
authors: X
authors: Liu
authors: Guangqian
authors: G
authors: Han
authors: Juntao
authors: J
authors: Zhao
authors: Jiaguo
authors: J
authors: Lv
authors: Youjun
authors: Y
authors: Zhou
mesh_terms: D000176:Acrosin / Q000037:antagonists & inhibitors* / Q000378:metabolism*; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D008958:Models, Molecular; D011485:Protein Binding; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D000096926:Benzenesulfonamides
chemical_list: D000176:Acrosin; D004791:Enzyme Inhibitors; D013449:Sulfonamides; D000096926:Benzenesulfonamides