New 4-[(1-benzyl-1H-indol-3-yl)carbonyl]-3-hydroxyfuran-2(5H)-ones, β-diketo acid analogs as HIV-1 integrase inhibitors

被引：31

作者：

Ferro, Stefania

Barreca, Maria Letizia

De Luca, Laura

Rao, Angela

Monforte, Anna Maria

Debyser, Zeger

Witvrouw, Myriam

Chimirri, Alba

机构：

[1] Univ Messina, Dipartimento Farmacochim, I-98168 Messina, Italy

[2] Katholieke Univ Leuven, B-3000 Louvain, Belgium

[3] IRC KULAK, Louvain, Belgium

来源：

ARCHIV DER PHARMAZIE | 2007年 / 340卷 / 06期

关键词：

HIV-1IN inhibitors; hydroxyfuran-2(5H)-ones; microwave-assisted synthesis; parallel synthesis; pharmacophore model;

D O I：

10.1002/ardp.200700066

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

In addition to our recent report on a series of rationally designed benzylindolyldiketo acids acting as potent HIV-1 integrase strand transfer inhibitors, we disclose the results obtained with novel compounds chemically modified on the diketo acid moiety in order to investigate its influence on the biological activity and cytotoxicity. The activity of designed and synthesized 4-[(1benzyl-1H-indol-3-yl)carbonyl]-3-hydroxyfuran-2(5H)-one derivatives lies in the micromolar range with regard to HIV IN enzymatic activity. The microwave-assisted synthesis was employed in some steps of the chemical procedures.

引用

页码：292 / 298

页数：7