Current Protocols
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2026
·Vol. 6
·期 4
·e70362
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IF 2.5
Zhuo-Yue Jia,Bin Wu,Wen-Wu Sun
This article describes an efficient acid-catalyzed cyclization strategy for constructing the tricyclic pyrimido[1,2-a]purin-10(3H)-one scaffold via the reaction of guanine derivatives with 1,1,3,3-tetramethoxypropane (TMOP) catalyzed by 2,4,5-trifluorobenzoic acid. The method features mild conditions, eliminates the need for hydroxyl protection, and exhibits excellent functional-group tolerance, making it applicable to the late-stage structural diversification of various nucleosides, nucleotides, and oligonucleotides. Using the antiviral drug acyclovir and an azide-containing guanosine derivative as model substrates, we successfully synthesized a tricyclic acyclovir analogue in 81% yield and an M 1 G-containing oligonucleotide in 40% yield. This protocol provides a general, convenient, and efficient experimental approach for synthesizing this class of potentially bioactive tricyclic nucleoside analogues. © 2026 Wiley Periodicals LLC. Basic Protocol 1 : Synthesis of tricyclic acyclovir analogue Basic Protocol 2 : Synthesis of M 1 G-containing oligonucleotide
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Biomaterials Science
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2020
·Vol. 8
·期 22
·6190-6203
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IF 6.183
Cheng-guang Wu,Xiang Wang,Yun-feng Shi,Bin-cheng Wang,Wei Xue,Yi Zhang
Supramolecular hydrogels derived from natural biomolecules have promising applications for drug delivery due to their inherent biocompatibility and tunable responsiveness to various stimuli. However, conventional hydrogels only modulate the release kinetics roughly to achieve sustained drug release, exhibiting fast-then-slow release behavior without on/off control. Herein, a guanosine (G)-quartet·Na+-borate supramolecular hydrogel (GB hydrogel) cross-linked via a guanosine–borate diester and intertwined by G4-nanofibres formed by π–π stacking of G4-quartets stabilized by Na+ is developed for on-demand release of Acyclovir (Acv). This GB hydrogel is facilely prepared by a one-pot hierarchical assembly involving hydrogen bonds, dynamic borate ester bonds and cation coordination, which endow it with tunable mechanical properties, excellent self-healing properties and reversible degradation behavior in response to pH, glucose and ion concentration. Benefiting from that the guanosine analog Acv is able to assemble into a G4-quartet by replacing guanosine via reversible hydrogen bonding, the Acv-loaded GB hydrogel showed favorable stability in physiological medium without undesired release and achieved external stimulus-triggered on-demand release with switchable on/off control and tunable release kinetics. Moreover, the GB hydrogel also exhibited excellent in vitro and in vivo biocompatibility. Such a natural nucleoside-based supramolecular hydrogel with on-demand drug release, self-healing property, biodegradability and biocompatibility provides a precisely controlled paradigm to overcome early burst release behavior of conventional hydrogels for the development of injectable hydrogel delivery systems.
研究领域:
药物递送
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生物材料
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化学
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COLLOIDS AND SURFACES B-BIOINTERFACES
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2018
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IF 3.997
Binge Deng,Xia Luo,Meng Zhang,Liming Ye,Yu Chen
Acyclovir (ACV) is a synthetic antiviral agent with serious side effect, particularly its nephrotoxicity, so this study was to explore the ultrasensitive detection of ACV by surface-enhanced Raman scattering (SERS). The enhancement capability of nanoparticles prepared by different chemical reduction were compared, and Ag nanoparticles reduced by citrate are the most propriate enhanced substrate for acyclovir. In addition, comparison between prominent SERS-enhanced bands and the precise mode descriptions predicted through density functional theory (DFT) simulations is used to understand the mechanisms between ACV and metallic surface. 130 different levels of ACV concentrations in a range from 10 −1 ∼10 -7 were used to build quantitative prediction models by two different modeling methods, partial least-squares (PLS) regression and artificial neural network (ANN). Under the optimal conditions, the performance of the PLS model was much better than ANN. The results demonstrated that SERS imaging with multivariate analysis holds great potential for the sensitive and cost effective clinic test of ACV and its metabolites in biological fluids.
研究领域:
药物分析
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生物医学工程
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化学计量学
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CRYSTAL GROWTH & DESIGN
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2023
·
IF 3.8
Fan-Zhi Bu,Yue-Ming Yu,Min Zhang,Cui-Wei Yan,Zhi-Yong Wu,Yan-Tuan Li
To achieve new breakthroughs in the development of synergistic antiviral medication cocrystals of acyclovir (AYL) with phenolic acids, a cocrystallization-driven strategy for optimizing the physicochemical properties and increasing the antiviral efficacy is proposed. This method emphasizes the structural features and medicinal value together with the dominant properties of gallic acid (GLA) to promote both solubility and permeability of AYL by cocrystallizing GLA into AYL’s lattice; meanwhile, the antiviral ability of ALY can be greatly increased by activating the antiviral potential of GLA and utilizing the synergistic antiviral activity of both in cocrystal formation. Guided by this idea, the first AYL-phenolic acid cocrystal, AYL-GLA-2H2O, is orientationally constructed and fully characterized. The accurate cocrystal structure revealed by single-crystal X-ray diffraction indicates that the entry of GLA into the AYL lattice has disrupted the homodimer of AYL itself, leading to the formation of a hydrophobic heterodimer between AYL and GLA molecules, coupled with an aqueous tetramer, thus endowing the cocrystal with both hydrophilic and hydrophobic characteristics. Such structural feature induces a concurrent enhancement in dissolubility and permeability of the cocrystal compared with the parent medicine. These observations can be strongly supported by density functional theory-based theoretical investigations involving molecular electrostatic potential, Hirshfeld surface, frontier molecular orbital, and Gibbs solvation free energy. Interestingly, the perfected AYL’s properties along with the stimulated antiviral activity of GLA enable the two ingredients in the cocrystal to display synergistic antiviral activity against the herpes simplex virus with a cooperativity index of less than 1, contributing to enhancing the antiviral ability. Thus, this contribution not only highlights the effectiveness of combining theory with experiment to solve AYL’s issues via the cocrystallization-driven method but fills in the gaps from previous studies on AYL-phenolic acid cocrystals with synergistic antiviral effects.
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FOOD CHEMISTRY
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2025
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IF 9.8
Wenxiu Zhou,Bingjie Li,Ke Xu,Shengman Zhang,Zhaoqian Li,Xin Wang
The residues of antiviral drugs acyclovir (ACV), penciclovir (PCV) and ganciclovir (GCV) in foods, particularly in ready-to-eat products, pose a significant threat to human health, making it urgent to develop a rapid and sensitive method for their detection. Herein, we designed a novel magnetic molecularly imprinted three-dimensional covalent organic framework (MICOF@Fe 3 O 4 ) for selective extraction of these antiviral drugs from complicated food matrix. The prepared MICOF@Fe 3 O 4 integrates molecular recognition ability, 3D COF structural advantages and magnetic responsiveness, providing high selectivity, large adsorption capacity and facile operation for magnetic solid-phase extraction (MSPE). Afterwards, a MSPE-UHPLC-MS/MS method was developed, which stands out as the most sensitive approach yet for ACV, PCV, GCV measurements and has been successfully applied to analyze thirteen ready-to-eat chicken samples. Endogenous PCV was detected in two of these samples, demonstrating the potential of the proposed method as a valuable tool for monitoring antiviral drug residues and ensuring food safety.
研究领域:
分析化学
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食品安全
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材料科学
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药物分析
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环境科学
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