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Synthesis and biological activity of novel 1H-1,4-diazepines containing benzene sulfonyl piperazine moiety
被引:11
|作者:
Saingar, Shalini
[1
]
Kumar, Rajesh
[2
]
Joshi, Yogesh Chandra
[1
]
机构:
[1] Univ Rajasthan, Dept Chem, Jaipur 302004, Rajasthan, India
[2] Def Lab, Jodhpur 342011, Rajasthan, India
关键词:
1H-1,4-diazepines;
beta-Diketones/beta-ketoesters;
Piperazine;
Silica sulphuric acid;
Ethylenediamine;
Biological activities;
PLATELET-ACTIVATING-FACTOR;
DRUG-RESISTANT STRAINS;
STAPHYLOCOCCUS-AUREUS;
DERIVATIVES;
ANTAGONISTS;
DESIGN;
POTENT;
1,4-DIAZEPINES;
ANTIFUNGAL;
AGENTS;
D O I:
10.1007/s00044-010-9430-2
中图分类号:
R914 [药物化学];
学科分类号:
100701 ;
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 beta-diketones/beta-ketoesters 5a-e were synthesized by the condensation reaction of [N (4)-(4-acetylamino) benzene sulfonyl) piperazinyl-N (1)-1-bromopropane with various beta-diketones/beta-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.
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页码:975 / 980
页数:6
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