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Nonnucleoside reverse transcriptase inhibitors (NNRTIs) nowadays represent very potent and most promising anti-AIDS agents that specifically target the HIV-1 reverse transcriptase (RT). However, the effectiveness of NNRTI drugs can be hampered by rapid emergence of drug-resistant viruses and severe side effects upon long-term use. Therefore, there is an(More)
A simple, rapid and sensitive sensing platform for the detection of As(III) has been fabricated in neutral media based on the mercaptoethylamine modified Au electrode. A wide detection range of 0.2-300 μg L(-1) and a low detection limit of 0.02 μg L(-1) were obtained with a preconcentration time of 100 s under optimal conditions. Compared with previous(More)
HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) nowadays represent most promising anti-AIDS drugs that specifically inhibit HIV-1 reverse transcriptase (RT). They have a unique antiviral potency, high specificity and low cytotoxicity. However, to a great extent, the efficacy of HIV-1 NNRTIs is compounded by rapid emergence of drug resistant(More)
Transcriptase Inhibitors: Lessons from the Development of Seven Representative Paradigms Dongyue Li,† Peng Zhan,† Erik De Clercq,‡ and Xinyong Liu*,† †Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, 44, West Culture Road, 250012, Jinan, Shandong, P. R. China ‡Rega Institute for Medical Research, K.U. Leuven,(More)
Highly luminescent and stable Cu nanoclusters (NCs) have been prepared, displaying an intriguing aggregation-induced emission (AIE) feature. The attractive AIE feature allowed the CuNCs to serve as pH stimuli-responsive functional materials. Additionally, we explored the utility of CuNCs for biosensing and catalysis applications.
In continuation of our efforts toward identification and optimization of novel non-nucleoside reverse transcriptase inhibitors (NNRTIs), we have employed a structure-based bioisosterism strategy, with which a new series of diarylpyridazine (DAPD) derivatives were synthesized and evaluated for their anti-HIV-1 (human immunodeficiency virus type 1) activity.(More)
A simple, rapid and portable electrochemical microchip sensing platform has been successfully constructed for chromium(VI) determination. Gold-silver-platinum (Au-Ag-Pt) three-material electrodes (gold as working electrode, silver as reference electrode and platinum as counter electrode) were integrated on one poly(methyl methacrylate) (PMMA) substrate by(More)
Guided by crystal structures of HIV-1 RT/DAPY complex and molecular modeling studies, a series of novel [1,2,4]triazolo[1,5-a]pyrimidine derivatives were rationally designed via structure-based core refining approach, synthesized through the readily accessible synthetic methods and evaluated for their anti-HIV activities in MT-4 cells. Preliminary(More)
In this work, we have developed a full-featured electrochemiluminescence (ECL) sensing platform based on a multichannel closed bipolar system. Owing to the three-channel and double-bipolar electrode (BPE) configuration, all the oxidants, reductants, or chemicals that are directly related to the ECL process can be detected in a single device, which greatly(More)
Currently, there has been considerable interest in the discovery of original molecules with broad-spectrum anti-HIV activity and favourable pharmacokinetic profiles, to be used as an alternative to the approved anti-HIV/AIDS drugs, should they fail as therapeutics. Five-membered azole heterocycles represent an important class of lead structures for novel(More)