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

来源：

JOURNAL OF HETEROCYCLIC CHEMISTRY | 2009年 / 46卷 / 06期

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.

引用

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页码：1420 / 1424

页数：5

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