Sepsis-associated acute kidney injury (AKI) management remains an unmet clinical need. SIRT5 inhibition shows renoprotective effects, suggesting its therapeutic potential. Using the cocrystal structure of SIRT5-lead compound 1, we rationally designed novel nitroethylene inhibitors that engage both the substrate and NAD+ binding sites. The optimized inhibitor 56 (IC50 = 0.29 μM) produced significant improvements in renal function (BUN and SCr) and histopathological damage in two models of septic AKI mice. Further mechanistic studies showed that the renoprotective effects are linked to the suppression of inflammation, which was demonstrated by reduced serum CRP and downregulated renal inflammatory cytokines (IL-6, MCP-1, TNF-α). Importantly, 56 showed no significant toxicity at the corresponding therapeutic dose. In summary, this study identifies a novel SIRT5 inhibitor and demonstrates its therapeutic potential against sepsis-associated AKI.

Supramolecular glasses are amorphous materials formed through non-covalent interactions between molecular building blocks. These interactions allow the formation of disordered but dynamic networks that differ from conventional inorganic or polymeric glasses. This chapter explores the fundamental concepts, design principles, and characterization methods that underpin the formation of supramolecular glasses. Key thermodynamic and kinetic factors that influence glass formation are discussed, along with the role of molecular design in controlling properties such as the glass transition temperature, optical transparency, and mechanical strength. The chapter also presents examples of small-molecule, oligomeric, and multicomponent systems that form supramolecular glasses, and outlines their potential use in flexible electronics, self-healing materials, and sustainable technologies. Future directions include the development of programmable supramolecular glasses that combine modularity, adaptability, and reprocessability, thereby bridging the gap between conventional glassy materials and dynamic soft matter.

Chiral recognition is a central tenet of life sciences and biomolecular interactions. It is indispensable for the enantiomeric analysis of pharmaceuticals and agrochemicals, as well as for the development of chiral materials and devices, with significant implications for biomedical applications. Despite its importance, the creation of efficient and highly selective enantiomer recognition in synthetic systems presents a major challenge. Supramolecular macrocycles address this by providing well-defined cavities and synergistically positioned functional groups, which enhance chiral selectivity and sensitivity beyond the capabilities of traditional small molecules. While the design and synthesis of macrocyclic hosts have advanced considerably, their practical utility is often constrained by their recognition efficiency, binding affinity, and their ability to recognize a diverse range of analytes. This article reviews recent chemical strategies for enhancing chiral complexation and recognition, and discusses the future outlook and obstacles within this field.

High-fidelity visualization of dynamic pH fluctuations in acidic and ultra-acidic microenvironments is imperative for elucidating pH-regulated pathophysiological processes. A critical challenge is the scarcity of robust near-infrared (NIR, >650 nm) fluorescent tools with tailored acidic pKa, large Stokes shifts, and exceptional stability under harshly acidic conditions for high-contrast imaging. To address this, we proposed trifluoromethyl molecular engineering on 9-alkylamino-Si-xanthene by adding a trifluoromethyl tail at the terminal of the 9-alkyl chain. This subtle structural modification induced surprising photophysical transformations: significant bathochromic shifts of 35-105 nm to ∼700 nm and dramatic pKa reduction from ∼8 to ∼4. The observed performance was rationalized through theoretical calculations, including HOMO-LUMO gaps, molecular electrostatic potential, natural population analysis, configuration changes, and Gibbs free energy difference. Utilizing the optimal probe SiNF2, we successfully observed enhanced lysosome-mitochondria communication during ferroptosis and achieved a striking 21.3-fold fluorescence contrast between cancer cells and normal cells. Notably, we demonstrate the first detection of diminished gastric acidity in an ethanol-induced gastric ulcer mouse model, highlighting the probe's potential for imaging-guided diagnosis and therapeutic monitoring of gastric disorders.

In search of novel fungicides, 35 target compounds were prepared through structural modifications at the phenolic hydroxyl, methyl, and nitro positions of 3,4-dimethyl-2,6-dinitrophenol. Several compounds exhibited promising antifungal activities against various phytopathogenic fungi, among which compound 5a demonstrated the most potent activity, with IC50 values of 0.67 mg/L against Rhizoctonia solani, 3.86 mg/L against Gibberella zeae, 2.64 mg/L against Pyricularia oryzae, 0.74 mg/L against Phytophthora infestans, 2.29 mg/L against Botrytis cinerea, and 3.75 mg/L against Ralstonia solanacearum. Compound 5a exhibited good in vivo preventive and therapeutic effects against Rhizoctonia solani and Pyricularia oryzae. Further mechanistic studies revealed that compound 5a and 2,4-dinitrophenol could increase mycelial cell membrane permeability, induce mycelial morphological shrinkage, and elevate intracellular reactive oxygen species levels, but there were significant differences in their effects. Moreover, the phytotoxicity of compound 5a on rice seed germination and its acute toxicity to zebrafish were significantly lower than those of fluazinam. These findings suggest that compound 5a holds promising potential for further development as antifungal agents.

Organic phosphate esters compounds, especially methyl-paraoxon (MP), pose a serious threat to the environment and human health. The development of robust organophosphorus hydrolases (OPHs)-like nanozymes to mimic natural enzymes is paramount for on-site monitoring MP. Herein, we reported a biomimetic engineering of highly active OPHs-like nanozymes through Zn-doped macrocyclic polyamine carbon dots (DOTA(Zn)-CDs). XPS confirmed ZnN coordination, while FTIR revealed macrocyclic polyamine frameworks with Zn-O/N coordination shifts, together mimicking the histidine‑zinc centers of native OPHs. This design induced a remarkable improvement in OPHs-like activity, demonstrated by a superior catalytic efficiency and a significant enhancement in adsorption affinity for MP hydrolysis, as confirmed by kinetic assays and density functional theory calculations. DOTA(Zn)-CDs nanozymes served as a dual-mode sensing platform, enabling the enhancement of detection performance. This system achieved a low detection limit of 1.55 μM and 2.57 μM for colorimetric and fluorescence detection of MP, alongside exceptional selectivity against interfering species and promising stability for 35 days. Finally, a portable DOTA(Zn)-CDs-based gelatin cube sensor was successfully constructed for practical, on-site detection. This work provides a fundamental strategy for designing efficient OPHs-like nanozymes by biomimetic active site engineering and underscores their significant potential for rapid environmental, agricultural and food detection.

Elevated selenium (Se) levels in water, particularly in its relative toxic Se(IV) form, pose significant risks to both ecosystems and human health, underscoring the urgent need for reliable on-site monitoring technologies. Miniaturized hydride generation/photochemical vapor generation-point discharge-optical emission spectrometers (HG/PVG-PD-OES) offer a promising solution for rapid field detection due to their compact size and low energy consumption. However, current systems suffer from insufficient sensitivity to meet increasingly stringent health regulations, as well as challenges related to cumbersome solid-phase preconcentration and desorption procedures. Herein, we developed a highly sensitive, field-deployable PD-OES platform for Se(IV) detection in water based on ethylation vapor generation coupled with purge-and-trap (P&T) preconcentration. This innovative approach achieved sensitivity enhancements of 17-fold and 3-fold compared to conventional HG and PVG methods, respectively. Under optimized conditions, the system achieved a detection limit of 1.8 mu g L- 1 for Se(IV) with a precision of 4.3 % (20 mu g L- 1, n = 11) based on Se atomic emission at 196.03 nm. The accuracy of the method was validated through the analysis of three Certified Reference Materials and three natural water samples, with recoveries ranging from 94 % to 106 %. This work presents a robust, non-chromatographic, fielddeployable platform for trace Se(IV) monitoring, meeting the growing demand for decentralized, high sensitivity environmental analysis tools.

Efficient macrocycle synthesis remains a persistently pursued objective in supramolecular chemistry. In this work, a series of chiral macrocycles (TBCHMs) incorporating Tröger’s base were synthesized via imine condensation reactions from Tröger’s base (TB) aldehyde derivatives and cyclohexane-1,2-diamines (CHDA). Gram-scale quantities of crystalline macrocycles were directly obtained during the process of their reaction. Precise modulation of macrocycle structural morphology was achieved by varying the chiral configuration of the components. Notably, chiral self-sorting was realized in these reaction systems, driven by the energy difference between diastereomers and their selective precipitation as crystals. This work might open up new insights for the modular preparation of chiral macrocycles based on dynamic covalent chemistry (DCC).

Sulfones are privileged structures, yet their synthesis heavily relies on toxic, waste-intensive oxidants. Adopting potent, greener oxidants like ozone (O3) offers sustainability, but inherent mass and heat transfer bottlenecks in batch reactors provoke hazardous accumulation and severe explosion risks. While continuous-flow technology safely harnesses these energetic oxidants, it exposes a kinetic paradox: within ultrashort, second-scale residence times, even ozone's intrinsic reactivity is insufficient, causing the oxidation to arrest prematurely at the sulfoxide intermediate. Herein, we report a robust and sustainable continuous-flow strategy enabled by Earth-abundant iron photocatalysis that unlocks the oxidative potential of ozone. This unique activation paradigm achieves the direct, highly selective oxidation of diverse sulfides to sulfones using exclusively an elemental oxygen-based oxidant within a mere 7-9 seconds. Using an inexpensive iron(iii) nitrate catalyst under visible light, the protocol's green credentials and robustness are demonstrated by its broad scope, gram-scale scalability, seamless catalyst recyclability, and successful application to pharmaceuticals, key drug intermediates, and novel herbicides. Mechanistic studies reveal that iron photocatalysis generates reactive oxygen species ((center dot)O2- and 1O2) in situ, effectively surmounting the kinetic barrier. This work offers an environmentally benign, efficient route to sulfones while conceptualizing a new paradigm for overcoming kinetic limitations in ultrafast flow chemistry.

Fluorophores with excellent emission often come at the cost of cell permeability, and this long‐standing dilemma has limited their effective applications in fluorescence bioimaging to some degree. We report a paradigm‐shifting discovery that carbonized polymer dots (CPDs) can function as a versatile, noncovalent translocation platform for a vast spectrum of otherwise impermeable fluorophores. Our investigation began with the serendipitous observation that a new molecule, 1‐(2‐hydroxyethyl)‐5‐oxo‐1,2,3,5‐tetrahydroimidazo[1,2‐a]pyridine‐7‐carboxylic acid (HECA), forms a stable, cell‐permeable nanocomplex with carbonized polymer dots (CPDs‐280) via noncovalent interactions (loading capacity ∼50.8%). This prompted a systematic exploration, which revealed that CPDs‐280 possess a remarkable capacity to override the innate targeting signals of diverse organelle‐specific dyes, rerouting them to the cytosol and demonstrating a carrier‐dominated localization mechanism. The platform's generality was rigorously proven by delivering custom‐designed, membrane‐impermeable amphiphilic dyes (ESY‐Na + and ESY), which remained inert alone but produced intense intracellular luminescence upon noncovalent complexation. This robust, cargo‐agnostic delivery capability is rooted in the abundant orthogonal anchor domains on the CPD's surface, enabling multimodal binding without chemical modification. This work unveils a generic strategy to breach biological barriers, instantly unlocking the vast repository of underutilized fluorescent probes for advanced bioimaging and theranostics.

Supramolecular catalysis uses noncovalent interactions,such as hydrogen bonding,π-π stacking,and host-guest recognition,to control reactivity and selectivity in chemical reactions[1,2].Un-like traditional covalent catalysis,supramolecular systems can cre-ate dynamic and adaptable microenvironments tailored to spe-cific substrates,similar to how enzymes work.This strategy has shown great promise in asymmetric catalysis,cascade reactions,and green chemistry applications.Recent advances focus on lever-aging less conventional noncovalent forces to expand the toolbox of supramolecular strategies in catalysis.

White-light organic molecules (WLOMs) exhibit distinct advantages over multi-component systems, such as good reproducibility and high long-term stability. However, the complex synthesis method and the unsatisfactory CIE coordinates hinder their further application. To meet this challenge, a series of novel white-light-emitting single-molecule compounds (BTP-Phs) based on the benzothiazolopyridinone skeleton were rationally designed and synthesized by modulating the donor-acceptor (D-A) structure of the molecules. The study of the structure-spectra relationship indicated that the strong electron-donating ability of the aromatic substituents and the synergistic effect of the extended pi-conjugated system enhanced the intramolecular charge transfer (ICT), which reduces the energy gap of the molecules and favors the long-wavelength emission of BTP-Phs. Notably, ideal white light emission (0.31, 0.34) was achieved through the aldehyde-gemdiol equilibrium in mixed solvents. The emission color could be finely tuned by solvent composition, excitation wavelength and concentration. In addition, a fluorescent ink was developed based on BTP-CHO-OPh as a functional material, which could realize information storage and encryption through QR codes or ASCII binary encoding. This study not only provides valuable design strategies for constructing WLOMs based on aldehyde-geminal diol equilibrium, but also highlights their potential in the field of secure information technology. (c) 2026 Published by Elsevier B.V. on behalf of Chinese Chemical Society and Institute of Materia Medica, Chinese Academy of Medical Sciences.

Amid the global pursuit of innovative approaches to disease di-agnosis and treatment,the interdisciplinary convergence of chem-istry and biomedicine has emerged as a pivotal force driving ad-vancements in the field.Cutting-edge technologies such as optical probes[1],nanotechnology[2],immunotherapy[3],and biosen-sors[4]are finding increasingly widespread application in dis-ease diagnosis and treatment,sustaining intense interest from both academia and industry.Against this backdrop,the 5th Xihua Chem-istry and Biomedicine Forum was successfully held at Xihua Uni-versity(Chengdu)from July 12 to 15,2025,infusing new vitality into academic exchanges and innovative progress in this domain.

Green and scalable nitration of aromatic compounds remains a challenge in chemical synthesis. While acid-free nitration using simple nitrogen oxides is highly attractive, it is often plagued by poor controllability, low efficiency, and safety hazards in conventional batch reactors. Building on the classical Kyodai nitration, we report a continuous-flow protocol that harnesses the synergy of nitrogen dioxide and ozone for the safe, acid-free, catalyst-free, and ultrafast nitration of arenes within seconds. This method demonstrates broad functional group tolerance and substrate scope, enabling the high-yield synthesis of diverse nitroarenes, encompassing the preparation of drug molecules, key pharmaceutical intermediates, and the late-stage functionalization of complex drugs. The protocol is readily scalable to the gram-scale and exhibits a significantly improved environmental performance over the batch process, as quantified by a substantially lower Process Mass Intensity (PMI). Kinetic studies support an electrophilic aromatic substitution (SEAr) mechanism. This work establishes a robust and scalable platform for green nitration, offering a compelling solution to a long-standing synthetic challenge.

Chiral sensing is crucial for understanding and controlling the biological activity of chiral molecule such as carbohydrates, amino acids, and proteins. It also plays a vital role in asymmetric synthesis, drug development, and the advancement of functional materials. Supramolecular macrocycle-based chiral sensors offer unique advantages over traditional small-molecule chiral sensors. This review highlights recent advancements in chiral sensing using supramolecular macrocycles, categorizing them into two primary groups: achiral and chiral macrocycles, based on their configurational features. Furthermore, it systematically outlines the synthetic strategies for these macrocycles, emphasizing their applications in chiral recognition and sensing.

Reactive oxygen species(ROS),including singlet oxygen(1O2),hydroxyl radicals(·OH),and superoxide anions(O2·-),are highly reactive molecules that play central roles in many chemical,bi-ological,and environmental processes due to their strong oxida-tive power[1].Generating ROS in a controlled manner under mild conditions is essential for achieving selective oxidation reac-tions.Light-driven methods are especially appealing for this pur-pose,as they offer precise control over where and when ROS are produced.

This manuscript outlines the Innovative Comprehensive Experimental Project (ICEP), which is highly interdisciplinary, practical, and relevant to current societal issues. The project serves as an excellent experimental teaching tool for graduate students of Chemistry, Pharmaceutical Engineering and other related majors. The experiment successfully combines the organic chemistry experimental techniques and bioactivity analysis skills learned by students during their undergraduate studies, which is vital for new graduate students to enhance their experimental proficiency. Through participating in hands-on training, students can not only effectively improve their ability to solve complex problems but also cultivate innovative thinking and scientific research competence in the process. The experiment begins with the pressing issue of bacterial drug resistance, prompting students to think critically about the relationship between bacterial resistance and the development of new antimicrobial drugs. This approach helps establish a proper method for using antimicrobial drugs. Throughout the experiment, students will synthesize 1,3,4-oxadiazole pleuromutilin molecules, evaluate their antimicrobial activity (in the Biosafety Level 2 laboratory), and simulate molecular docking. The interactive teaching method between teachers and students runs throughout the preparation, implementation, and summary parts of the project. This approach positively impacts students' theoretical knowledge expansion, practical skill enhancement, and innovation ability cultivation.

This study introduces a novel strategy for utilizing amides as direct alkylating agents. The activation of amides with Tf2O and 2-F-Py induces the migration of the alkyl group from the nitrogen of the amide to the nitrogen of 2-F-Py. Following a one-pot hydrolysis or reduction step, N-substituted 2-pyridones or tetrahydropyridines are generated in situ. A total of 34 related compounds were synthesized with high yields across various substrates. This methodology was further applied to the synthesis of key intermediates for C3a receptor inhibitors. Mechanistic studies indicate the formation of a pyridinium salt as a reactive intermediate in the process. Overall, this work presents a novel approach to the application of amides in synthetic chemistry.

White-light emitting organic materials have garnered significant attention due to their potential applications in lighting and display technologies. Compared to systems that emit distinct colors by combining multiple molecules, single-molecule white-light emission systems offer notable advantages, such as simple preparation, good repeatability and stability. In this study, a novel fluorescent molecule (BTP-CHO) was developed. For the first time, a single-molecule near-white light emission system by exploiting the internal equilibrium of aldehyde-gemdiol in water of BTP-CHO was constructed. BTP-CHO exists predominantly as the aldehyde form in DMSO and shows green fluorescence; while BTP-CHO shows blue fluorescence because of the internal equilibrium of aldehyde-gemdiol in water. Polychromatic photoluminescence could be achieved by fine-tuning various parameters, including excitation wavelength and solvent ratio. Additionally, we synthesized three derivatives of BTP-CHO for further investigating the universality of this strategy and the results indicate that the strategy has good universality. Finally, BTP-CHO was successfully applied in the development of information encryption and near-white light hydrogels. This work provides new insights into the design of organic single-molecule white-light emitters and broadens the scope of research on aldehyde-gemdiol intrinsic equilibrium about white-light emitting.