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
收藏
页码：228 / 234
页数：7
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