Synthesis and acrosin inhibitory activity of substituted 4-amino-N-(diaminomethylene) benzenesulfonamide derivatives

Bioorg Med Chem Lett. 2011 Nov 15;21(22):6674-7. doi: 10.1016/j.bmcl.2011.09.060. Epub 2011 Sep 21.

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acrosin / antagonists & inhibitors*
  • Acrosin / metabolism*
  • Benzenesulfonamides
  • Enzyme Inhibitors / chemical synthesis
  • Enzyme Inhibitors / chemistry*
  • Enzyme Inhibitors / pharmacology*
  • Humans
  • Models, Molecular
  • Protein Binding
  • Structure-Activity Relationship
  • Sulfonamides / chemical synthesis
  • Sulfonamides / chemistry*
  • Sulfonamides / pharmacology*

Substances

  • Enzyme Inhibitors
  • Sulfonamides
  • Acrosin