Synthesis of New Pyridazine Derivatives as Potential Anti-HIV-1 Agents

被引:4
|
作者
Ferro, Stefania [1 ]
Agnello, Stefano [1 ]
Barreca, Maria Letizia [2 ]
De Luca, Laura [1 ]
Christ, Frauke [3 ,4 ]
Gitto, Rosaria [1 ]
机构
[1] Univ Messina, Dept Med Chem, I-98168 Messina, Italy
[2] Univ Perugia, Dept Pharmaceut Chem & Technol, I-06123 Perugia, Italy
[3] Katholieke Univ Leuven, B-3000 Louvain, Belgium
[4] IRC KULAK, B-3000 Louvain, Belgium
关键词
HIV-1 INTEGRASE INHIBITORS; STRAND-TRANSFER INHIBITORS;
D O I
10.1002/jhet.230
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
We herein report conventional and microwave-assisted methods for the synthesis of a series of compounds containing some bivalent ion chelating requirements useful to exert potential HIV-1 integrase (IN) enzyme inhibition activity. The biological screening highlighted that only derivative 5 proved to be a strand-transfer step inhibitor of the virus integration process at micromolar concentration.
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页码:1420 / 1424
页数:5
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