Novel Thiazolidinone Derivatives with an Uncommon Mechanism of Inhibition Towards HIV-1 Reverse Transcriptase

被引：21

作者：

Pitta, Eleni ^{[2
]}

Crespan, Emmanuele ^{[1
]}

Geronikaki, Athina ^{[2
]}

Maga, Giovanni ^{[1
]}

Samuele, Alberta ^{[1
]}

机构：

[1] CNR, IGM, I-27100 Pavia, Italy

[2] Aristotle Univ Thessaloniki, Sch Pharm, Thessaloniki 54124, Greece

来源：

LETTERS IN DRUG DESIGN & DISCOVERY | 2010年 / 7卷 / 04期

关键词：

HIV-1; RT; HAART; NNRTIs; AIDS; Antiretroviral therapy; Enzyme kinetics; DRUG-RESISTANCE; AGENTS; DESIGN; INFECTION; NNRTIS;

D O I：

10.2174/157018010790945869

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Here, we show that novel 2-aryl-3-(4-adamantyl-thiazol-21,3-thiazolidin-4-one derivatives have a mixed- or fully competitive mechanism of inhibition towards HIV-1 Reverse Transcriptase with respect to the substrates of the reaction. Thus, they are interesting starting points for the development of novel NNRTIs with an uncommon mechanism of action.

引用

页码：228 / 234

页数：7

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