EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
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2023
·
IF 6.7
Ziwen Zhang,Shi-Long Zhang,Chengyao Wu,Huan-Huan Li,Liang Zha,Jingbo Shi,Xinhua Liu,Hua-Li Qin,Wenjian Tang
SuFEx click chemistry has been a method for the rapid synthesis of functional molecules with desirable properties. Here, we demonstrated a workflow that allows for in situ synthesis of sulfonamide inhibitors based on SuFEx reaction for high-throughput testing of their cholinesterase activity. According to fragment-based drug discovery (FBDD), sulfonyl fluorides [R–SO 2 F] with moderate activity were identified as fragment hits, rapidly diversified into 102 analogs in SuFEx reactions, and the sulfonamides were directly screened to yield drug-like inhibitors with 70-fold higher potency (IC 50 = 94 nM). Moreover, the improved molecule J8-A34 can ameliorate cognitive function in A β 1−42 -induced mouse model. Since this SuFEx linkage reaction succeeds on picomole scale for direct screening, this methodology can accelerate the development of robust biological probes and drug candidates.
研究领域:
化学
·
药物发现
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神经科学
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DOI
PubMed
高影响因子
Polymer Chemistry
·
2019
·Vol. 11
·期 5
·1033-1042
·
IF 4.76
Haibo Wan,Shiyuan Zhou,Peiyang Gu,Feng Zhou,Da Lyu,Qinghua Xu,Anna Wang,Haibin Shi,Qingfeng Xu,Jianmei Lu
Three polysulfates P1, P2 and P3 containing two representative AIE-active groups, tetraphenyl ethylene and naphthylamide, were successfully synthesized based on a sulfur(VI) fluoride exchange (SuFEx) click reaction. Their solid fluorescence was studied in detail and liquid fluorescence emission could be tuned by choosing solvents with different polarities. P1 with a branched structure showed higher fluorescence emission than P2 and P3 both in the solid state and in organic solutions because of the more crowded local environment of the tetraphenyl ethylene group in the main chain. Moreover, all the polymers exhibited typical aggregation induced emission (AIE) effects in the solid state and in DMF/water solutions. Furthermore, their two-photon fluorescence behaviours were similar to their one-photon fluorescence behaviours in different organic solvents and in 90% DMF/water solutions. Interestingly, they could selectively detect cyanide ions with lower detection limits in water on account of the anion–π interactions between the naphthylamide groups and the cyanide ions. The detection limits of P1 (0.137 μM) and P2 (0.131 μM) are lower than P3 (0.145 μM), which may be attributed to the more exposed active sites of the P1 and P2 nanoparticles (NPs). All the results indicate that these polymers have higher sensitivity and better applicability for cyanide ion detection in water and in living cells.
研究领域:
材料科学
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生物医学
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产品关联
DOI
高影响因子
APPLIED SURFACE SCIENCE
·
2023
·
IF 6.7
Yijia Yu,Shengjie Liu,Wenjuan Xia,Zhichen Zhu,Wenjin Wang,Chuanjiang Zhou,Zhaoqiang Wu,Hong Chen
To meet the development of multifunctional surfaces with long-term antibacterial activity for biomaterials and implantable devices, herein, a novel self-polishing antibacterial surface was developed. The functionalized surface was prepared by first surface-initiated ring-opening grafting polymerization (SI-ROP) of a cyclic carbonate monomer 4′-(fluorosulfonyl)benzyl-5-methyl-2-oxo-1,3-dioxane-5-carboxylate (FMC) containing a sulfonyl fluoride group in the side chain onto the material surface and then by a “sulfur(IV)-fluorine” exchange (SuFEx) postclick modification reaction to link the imidazolium salt ionic liquid to the polyFMC (PFMC) brush. In vitro experimental results showed that the functionalized surface has good biocompatibility, enzymatic biodegradable properties and excellent bactericidal properties, which can effectively kill E. coli (∼94%) and S. aureus (∼93%). In addition, the functionalized surface can release the killed bacteria (∼90%) several times efficiently under the action of lipase enzymatic degradation, restoring the original bactericidal function of the surface, thus forming a dynamic self-polishing and self-renewing antibacterial surface. Therefore, this method for the fabrication of self-polishing antibacterial surfaces may offer innovative insights into applications of biomedical implant materials.
研究领域:
材料科学
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生物医学工程
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表面化学
·
抗菌技术
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产品关联
DOI
高影响因子
COLLOIDS AND SURFACES B-BIOINTERFACES
·
2024
·
IF 5.4
Yijia Yu,Wenjuan Xia,Wenjin Wang,Zhaoqiang Wu,Hong Chen
Hydrophilic antifouling polymers provide excellent antifouling effects under usual short-term use conditions, but the long-term accumulation of contaminants causes them to lose their antifouling properties. To overcome this drawback, surface-initiated ring-opening graft polymerization (SI-ROP) was performed on the surface of the material by applying the cyclic carbide monomer 4′-(fluorosulfonyl)benzyl-5-methyl-2-oxo-1,3-dioxane-5-carboxylate (FMC), which contains a sulfonylfluoride group on the side chain, followed by a “sulfur(IV)-fluorine exchange” (SuFEx) post click modification reaction to link the hydrophilic polyethylene glycol (PEG) to the polyFMC (PFMC) brush, and a novel antifouling strategy for self-polishing dynamic antifouling surfaces was developed. The experimental results showed that the antifouling surface could effectively prevent the adsorption of proteins such as bovine serum albumin (BSA, ∼96.4%), fibrinogen (Fg, ∼87.8%) and lysozyme (Lyz ∼69.4%) as well as the adhesion of microorganisms such as the bacteria Staphylococcus aureus ( S. aureus ) (∼87.5%) and HeLa cells (∼67.2%). Moreover, the enzymatically self-polished surface still has excellent antifouling properties. Therefore, this modification method has potential applications in the field of biosensors and novel antifouling materials.
研究领域:
材料科学
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表面化学
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生物医学工程
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高分子科学
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生物材料
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF POLYMER SCIENCE
·
2022
·Vol. 60
·期 13
·1954-1961
·
IF 3.046
Jingrui Liu,Wei Sun,Zhaoqiang Wu,Hong Chen
A novel trithiocarbonate reversible addition−fragmentation chain transfer (RAFT) reagent, 3-azidopropyl (4-[fluorosulfonyl]benzyl)trithiocarbonate (Az-FSBCT), which has both clickable azidopropyl and sulfonyl fluoride moieties, was designed and synthesized. Using the RAFT agent Az-FSBCT and triethylboron as an initiator, well-defined poly( N -vinylpyrrolidone) (PVP), in which the azide and sulfonyl fluoride groups are at the α and ω positions of the polymer chains, were prepared without prior deoxygenation at room temperature. Moreover, the possibilities for the construction of new functionalized polymers were also demonstrated by a “click” copper(I)-catalyzed alkyne-azide cycloaddition (CuAAC) and sulfur(VI)-fluoride exchange (SuFEx) postreaction using these terminal functional PVPs. Graphical
研究领域:
高分子化学
·
材料科学
·
有机化学
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产品关联
DOI
高影响因子
危险品化学品经营许可证（带存储）