Design, Synthesis, and Biological Evaluation of 1,3,4-Thiadiazole Derivatives as Novel Potent Peptide Deformylase Inhibitors for Combating Drug-Resistant Gram-Positive and -Negative Bacteria.

The prevalence of drug-resistant bacteria is a major challenge throughout the world, especially with respect to Gram-negative bacteria, such as drug-resistant , which are regarded as the greatest bacterial threat to human health by the World Health Organization (WHO). In this work, 1,3,4-thiadiazole was introduced into the main skeleton of the classical peptidomimetic peptide deformylase (PDF) inhibitor in pursuit of highly efficient and broad-spectrum bacteriostatic drugs. Upon detailed structure-activity relationship study, PDF inhibitors that possess satisfactory activity against both Gram-positive and Gram-negative bacteria as well as a lower potential for methemoglobin toxicity were screened out.

R2R3-MYB transcription factors RrMYB12 and RrMYB111 regulate the accumulation of flavonols and anthocyanins.

Roses () are a famous flower with high ornamental and economic value. But the petals of roses are usually pink and purple, which restricted its application in garden settings. Flavonols and anthocyanins are crucial secondary metabolites related to flower pigmentation in plants.

Adhesive and antibacterial guar gum-based nanocomposite hydrogel for remodeling wound healing microenvironment.

Hydrogels are promising wound dressings due to their extracellular matrix-like properties and tunable structure-function characteristics. Besides the physical isolation effect, hydrogel dressings are highly expected to possess tissue-adhesive performance and antibacterial capacity, which are beneficial for their clinical translations. Herein, a guar gum (GG)-based nanocomposite hydrogel was fabricated by mixing methacrylated GG (GGMA), acrylic acid, acrylated 3-aminophenylboronic acid, mangiferin (MF)-loaded cetyltrimethyl ammonium chloride (CTAC) micelles (MF@CTAC) and radical initiator.

Antibacterial carboxymethyl chitosan hydrogel loaded with antioxidant cascade enzymatic system for immunoregulating the diabetic wound microenvironment.

Diabetic wound healing faces several complex challenges, such as hypoxia, oxidative stress, and bacterial infections, which severely inhibit the wound-healing process. Herein, a quaternary ammonium salt-crosslinked carboxymethyl chitosan hydrogel (TPC) with excellent antioxidant and antibacterial properties was developed to immunoregulate the diabetic wound microenvironment. The TPC hydrogel was prepared by first mixing carboxymethyl chitosan (CMCS) and protocatechualdehyde (PA), followed by the addition of a quaternary ammonium cross-linker (TSPBA) and a superoxide dismutase (SOD)-catalase (CAT) cascade system.

Integrating Umpolung and CO Shuttling Strategies for the Synthesis of C- and C-α-Ketoacids from Aldehydes.

The direct carboxylation of aldehydes with CO is rare due to the polarity mismatch between these two electrophilic substrates. To address this challenge, we propose a sequential approach for synthesizing α-ketoacids from commercially available aldehydes by integrating umpolung and CO shuttling strategies. This transition metal-free shuttle carboxylation method enables the transfer of CO from triphenylacetic acid potassium salt to thioacetal, eliminating the need for handling pressurized CO gas or using specialized equipment, while also enhancing the reaction's functional group tolerance.

Photoredox-Catalyzed Carbamoyl Radical-Initiated Dearomative Spirocyclization To Access Spiro-Cyclohexadiene Oxindoles.

The sustainable construction of spirocyclic compounds is important to the scientific community and the pharmaceutical industries. Herein, we demonstrate a carbamoyl radical-initiated intramolecular dearomative spirocyclization to access the spiro-cyclohexadiene oxindoles under visible light irradiation, which constitutes the first example of accessing the I-substituted derivatives that facilitate diversified transformations. Additionally, the scalability, late-stage modification of drugs, and significant antitumor activity of the products demonstrate the novel spirocyclic synthesis platform for expediting drug development.

From agricultural waste residue to wealth support: A magnetically N-heterocyclic carbene functionalized corn cob cellulose as a new stabilizer for Pd catalyst in Suzuki reaction.

Because of eco-friendliness, biodegradability and ease of modification, cellulose is deemed as alternative to unrenewable petroleum resources. Nonetheless, it is more indispensable to exploit corn cob cellulose produced from agricultural waste residue as supportive materials in green catalysis. In this study, a new magnetically benzimidazole functionalized cellulose/FeO derived from corn cob cellulose as a stabilizer agent (FeO@CL-NHC) was prepared, and palladium was immobilized on this stabilizer (FeO@CL-NHC-Pd).

Concomitant genomic features stratify prognosis to patients with advanced EGFR mutant lung cancer.

This study aimed to explore the clinical significance of genomics features including tumor mutation burden (TMB) and copy number alteration (CNA) for advanced EGFR mutant lung cancer. We retrospectively identified 1378 patients with advanced EGFR mutant lung cancer and next-generation sequencing tests from three cohorts. Multiple co-occurring genomics alternations occurred in a large proportion (97%) of patients with advanced EGFR mutant lung cancers.

A Tumor-Targeting Dual-Modal imaging probe for nitroreductase in vivo.

Nitroreductase (NTR) overexpression often occurs in tumors, highlighting the significance of effective NTR detection. Despite the utilization of various optical methods for this purpose, the absence of an efficient tumor-targeting optical probe for NTR detection remains a challenge. In this research, a novel tumor-targeting probe (Cy-Bio-NO) is developed to perform dual-modal NTR detection using near-infrared fluorescence and photoacoustic techniques.

Direct C-H Alkylation of Benzothiadiazoles via Organic Photoredox Catalysis.

2,1,3-Benzothiadiazole is widely used as a privileged scaffold in pharmaceuticals and organic functional materials. Nonetheless, many current methods for the functionalization of 2,1,3-benzothiadiazole rely on preactivation, transition metal catalysts/promoters, or an elevated reaction temperature. Herein we disclose a transition-metal-free visible-light-induced photocatalytic method for the direct C-H alkylation of 2,1,3-benzothiadiazole using readily accessible carboxylic acid derivatives, i.

Evaluation of Loquat Jam Quality at Different Cooking Times Based on Physicochemical Parameters, GC-IMS and Intelligent Senses.

The study compared and analyzed the quality of loquat jam with different cooking times through physicochemical parameters, headspace-gas chromatography-ion migration spectroscopy (HS-GC-IMS) and intelligent senses. The results showed that with the prolongation of the cooking time, the color of loquat jam slowly deepened, the energy significantly increased, the adhesiveness, gumminess, hardness and chewiness enhanced, the free amino acid content increased from 22.40 to 65.

Synthesis of 1,7-Fused Indolines Tethered with Spiroindolinone Based on C-H Activation Strategy with Air as a Sustainable Oxidant.

Herein, we present an efficient synthesis of 1,7-fused indolines tethered with a spiroindolinonyl moiety through the cascade reaction of indolin-1-yl(aryl)methanimines with diazo oxindoles. To the best of our knowledge, this is the first example in which 1,7-fused indoline skeleton was constructed along with the simultaneous introduction of a spiro element initiated by the C-H bond activation of indoline. In forming the title product, the indoline substrate and the diazo coupling partner demonstrated an unprecedented reaction pattern in which the latter acts as a C1 synthon to participate in the construction of the spirocyclic scaffold through the reductive elimination of a key seven-membered Ru(II) species by using air as an effective and sustainable oxidant to regenerate the active catalyst.

A guanosine/konjac glucomannan supramolecular hydrogel with antioxidant, antibacterial and immunoregulatory properties for cutaneous wound treatment.

Developing naturally-derived wound dressing materials with intrinsic therapeutic effects is desirable for the clinical applications. Recently, guanosine-based supramolecular G-quadruplex (G4) hydrogel exhibited great potential in preparing biological materials due to its simple fabrication method and responsive gel networks. However, the weak mechanical properties and the consequent burst release of bioactive molecules restrict its clinical applications.

Photocatalytic Umpolung Strategy for the Synthesis of α-Amino Phosphine Oxides and Deuterated Derivatives.

Direct, economical, and green synthesis of deuterated α-amino phosphine oxides remains an elusive challenge in synthetic chemistry. Herein, we report a visible-light-driven umpolung strategy for synthesizing deuterated α-amino phosphine oxides from isocyanide using 1,2,3,5-tetrakis(carbazol-9-yl)-4,6-dicyanobenzene as the photocatalyst and DO as the deuterium source. Moreover, the streamlined and sustainable methodology can be applied in the modification of amino acids, natural products, and drugs.

Body temperature-induced adhesive hyaluronate/gelatin-based hybrid hydrogel dressing for promoting skin regeneration.

Skin wound management faces significant clinical challenges, including continuous bacterial infection and inflammation. Therefore, developing removable hydrogel dressings with intrinsic multifunctional properties is highly desirable. In this study, a body temperature-induced adhesive and removable hydrogel was designed to treat skin defect wounds.

A serial mediation model of negative life events on school adjustment of left-behind adolescents in rural china: the central role of hope and gratitude.

Adjustment difficulties of school students are common and their school adjustment has gained wide concern in recent years. Negative life events (NLEs) hope, and gratitude have been associated with school adjustment. However, the potential effect of NLEs on hope and gratitude and whether hope and gratitude mediate the association between NLEs and school adjustment among high students have not been studied.

Cascade enzymatic preparation of carboxymethyl chitosan-based multifunctional hydrogels for promoting cutaneous wound healing.

Designing wound dressings with inherent multifunctional therapeutic effects is desirable for clinical applications. Herein, a series of multifunctional carboxymethyl chitosan (CMCS)-based hydrogels were fabricated by the facile urate oxidase (UOX)-horseradish peroxidase (HRP) cascade enzymatic crosslinking system. For the first time, the cascade enzymatic crosslinking system was not only used for preparing hydrogel wound dressings but also for accelerating wound healing due to the activity retention of the self-compartmental enzymes.

Dual-Atom Catalysts Derived from a Preorganized Covalent Organic Framework for Enhanced Electrochemical Oxygen Reduction.

Dual-atom catalysts (DAC) are deemed as promising electrocatalysts due to the abundant active sites and adjustable electronic structure, but the fabrication of well-defined DAC is still full of challenges. Herein, bonded Fe dual-atom catalysts (Fe DAC) with Fe N C O configuration were developed through one-step carbonization of a preorganized covalent organic framework with bimetallic Fe chelation sites (Fe COF). The transition from Fe COF to Fe DAC involved the dissociation of the nanoparticles and the capture of atoms by carbon defects.

Schiff base modified starch: A promising biosupport for palladium in Suzuki cross-coupling reactions.

Starch can be used in diverse fields because it is a readily available, non-toxic polysaccharide with adaptable functionality and biodegradability. In this study, taking the aforementioned characteristics into consideration, we designed a modified starch (Starch-SB), which serves as supporting material for palladium stabilization. This new air and moisture-stable robust palladium composite [Starch-SB-Pd(II)] was characterized by FT-IR, XRD, TGA, XPS, SEM, EDX, TEM, CP/MAS C NMR, and ICP-MS analytical techniques.

Honokiol@PF127 crosslinked hyaluronate-based hydrogel for promoting wound healing by regulating macrophage polarization.

Bacterial infection, oxidative stress and inflammation are the main obstacles in wound healing. Hydrogels with moist and inherent properties are beneficial to wound healing. Here, we fabricated a honokiol-laden micelle-crosslinked hyaluronate-based hydrogel by simply mixing honokiol-laden PF127-CHO micelles, 3,3'-dithiobis(propionohydrazide) grafted hyaluronic acid and silver ions.

Ultrathin Two-Dimensional BiOCl-Bi S -Cu S Ternary Heterostructures with Enhanced LSPR effect for NIR Photonic Bacterial Disinfection.

Photonic disinfection, particularly near-infrared (NIR) light triggered antibacterial, has emerged as a highly promising solution for combating pathogenic microbes due to its spatiotemporal operability, safety, and low cost of apparatus. However, it remains challenging to construct NIR-responsive antibacterial agents with high light-converting efficacy and elucidate synergistic mechanisms. In this work, ultrathin two-dimensional (2D) BiOCl-Bi S -Cu S ternary heterostructures that can efficiently kill drug-resistant bacteria were synthesized by doping 0D Bi S and Cu S nanoparticles in the 2D BiOCl nanosheets via a facile one-pot hydrothermal method.

Heterojunction structured BiOCl-BiS nanosheets as mitochondria-targeted near-infrared photothermal and photodynamic therapy agent.

Mitochondria-targeted phototherapy, especially combined photothermal therapy (PTT) and photodynamic therapy (PDT), has been regarded as an attractive strategy for the treatment of tumor. In this study, a facile approach to prepare two-dimensional (2D) BiOCl-BiS nanostructures was developed, where BiS quantum dots were doped in/on the ultrathin BiOCl nanosheets, forming a p-n heterojunction. The BiOCl-BiS shows favorable photothermal conversion efficiency (32%) and synergistically reactive oxygen species (ROS) generating capability under near-infrared (NIR) irradiation.