Synthesis and biological activity of novel 1H-1,4-diazepines containing benzene sulfonyl piperazine moiety

摘要

The synthesis of biologically active 1H-1,4-diazepines 6a–e in good yield, from the heterocyclization reaction of [N 4-(4-acetylamino) benzene sulfonyl) piperazinyl-N 1-propyl]-1,3-dialkyl/aryl propane-1,3-dione 5a–e and ethylenediamine (EDA) in the presence of silica sulphuric acid (SSA) is described. The novel β-diketones/β-ketoesters 5a–e were synthesized by the condensation reaction of [N 4-(4-acetylamino) benzene sulfonyl) piperazinyl-N 1-1-bromopropane with various β-diketones/β-ketoesters 4a–e. All structures of the newly synthesized compounds were elucidated by elemental analysis and spectral studies. The compounds 6a–e have been screened for antimicrobial, antifungal and anthelmintic activity.