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1.
Front Microbiol ; 15: 1296059, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38322313

RESUMO

Objective: This study aimed to evaluate the clinical value of dynamic monitoring of neutrophil/lymphocyte ratio (NLR), APACHE II (Acute Physiology and Chronic Health Evaluation II) score, and Sequential Organ Failure Assessment (SOFA) score in predicting 28-day prognosis and drug resistance in patients with bloodstream infection with Acinetobacter baumannii-calcoaceticus complex (Abc complex). Patients and methods: In this research, individuals admitted to Tianjin Medical University General Hospital from January 2017 to March 2023 with bloodstream infections and a minimum of one Abc complex positive blood culture were chosen. The risk factors for the 28-day prognosis and drug resistance were analyzed using logistic regression. The NLR, APACHE II score, and SOFA score were evaluated for predicting 28-day prognosis and drug resistance using an ROC curve analysis. The data were analyzed using R Studio to find correlations and conduct survival analysis with the Kaplan-Meier method. Results: The final statistical analysis included a total of 129 patients with bloodstream infections caused by Abc complex. Independent risk factors predicting mortality within 28 days were identified as follows: the SOFA score and APACHE II scores at 24 h, and APACHE II scores at 72 h after the onset of blood infection (p < 0.05). NLR, SOFA score, and APACHE II score did not predict drug resistance. Patients with Carbapenem-resistant Acinetobacter baumannii-calcoaceticus complex (CRAB) had shorter survival times than those with carbapenem-sensitive strains (40.77 days vs. 47.65 days, respectively, p = 0.0032). Conclusion: The prognosis of Abc complex bloodstream infection is affected by both SOFA and APACHE II scores. Both scoring systems have similar prognostic values at different time points after infection, but for computational convenience, it is recommended to use the SOFA score. NLR exhibits limited effectiveness in predicting mortality within 28 days. Carbapenem-resistant individuals with Abc complex experience significantly reduced survival time. None of the three factors-SOFA score, APACHE II score, and NLR-can early predict the occurrence of CRAB infections effectively.

2.
Front Public Health ; 12: 1148705, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38327578

RESUMO

Objectives: The present study analyzed the impact of the COVID-19 pandemic on the prevalence and incidence of new leprosy cases, as well as the diversity, distribution, and temporal transmission of Mycobacterium leprae strains at the county level in leprae-endemic provinces in Southwest China. Methods: A total of 219 new leprosy cases during two periods, 2018-2019 and 2020-2021, were compared. We genetically characterized 83 clinical isolates of M. leprae in Guizhou using variable number tandem repeats (VNTRs) and single nucleotide polymorphisms (SNPs). The obtained genetic profiles and cluster consequences of M. leprae were compared between the two periods. Results: There was an 18.97% decrease in the number of counties and districts reporting cases. Considering the initial months (January-March) of virus emergence, the number of new cases in 2021 increased by 167% compared to 2020. The number of patients with a delay of >12 months before COVID-19 (63.56%) was significantly higher than that during COVID-19 (48.51%). Eighty-one clinical isolates (97.60%) were positive for all 17 VNTR types, whereas two (2.40%) clinical isolates were positive for 16 VNTR types. The (GTA)9, (TA)18, (TTC)21 and (TA)10 loci showed higher polymorphism than the other loci. The VNTR profile of these clinical isolates generated five clusters, among which the counties where the patients were located were adjacent or relatively close to each other. SNP typing revealed that all clinical isolates possessed the single SNP3K. Conclusion: COVID-19 may have a negative/imbalanced impact on the prevention and control measures of leprosy, which could be a considerable fact for official health departments. Isolates formed clusters among counties in Guizhou, indicating that the transmission chain remained during the epidemic and was less influenced by COVID-19 preventative policies.


Assuntos
COVID-19 , Hanseníase , Humanos , Mycobacterium leprae/genética , Pandemias , DNA Bacteriano/genética , COVID-19/epidemiologia , Hanseníase/epidemiologia , Hanseníase/microbiologia , China/epidemiologia
3.
Artigo em Inglês | MEDLINE | ID: mdl-38321212

RESUMO

Cholangiocarcinoma (CCA) is a type of malignant tumor originating from the intrahepatic, periportal, or distal biliary system. The treatment means for CCA is limited, and its prognosis is poor. Spatholobi Caulis (SC) is reported to have effects on anti-inflammatory and anti-tumor, but its role in CCA is unclear. First, the potential molecular mechanism of SC for CCA treatment was explored based on network pharmacology, and the core targets were verified by molecular docking and molecular dynamics simulation. Then, we explored the inhibitory effect of SC on the malignant biological behavior of CCA in vitro and in vivo and also explored the related signaling pathways. The effect of combination therapy of SC and cisplatin (DDP) in CCA was also explored. Finally, we conducted a network pharmacological study and simple experimental verification on luteolin, one of the main components of SC. Network pharmacology analysis showed that the core targets of SC on CCA were AKT1, CASP3, MYC, TP53, and VEGFA. Molecular docking and molecular dynamics simulation indicated a good combination between the core target protein and the corresponding active ingredients. In vitro, SC inhibited proliferation, migration, invasion, and epithelial-mesenchymal transition (EMT) of CCA cells. In vivo experiments, the results were consistent with in vitro experiments, and there was no significant hepatorenal toxicity of SC at our dosage. Based on KEGG enrichment analysis, we found PI3K/AKT signaling pathway might be the main signaling pathway of SC action on CCA by using AKT agonist SC79. To explore whether SC was related to the chemotherapy sensitivity of CCA, we found that SC combined with DDP could more effectively inhibit the progression of cholangiocarcinoma. Finally, we found luteolin may inhibit the proliferation and invasion of CCA cells. Our study demonstrates for the first time that SC inhibits the progression of CCA by suppressing EMT through the PI3K-AKT signaling pathway, and SC could enhance the effectiveness of cisplatin therapy for CCA.

4.
J Imaging Inform Med ; 2024 Feb 06.
Artigo em Inglês | MEDLINE | ID: mdl-38321312

RESUMO

Panoramic radiography imaging plays a crucial role in the diagnostic process of dental diseases. However, current artificial intelligence research datasets for panoramic radiography dental image processing are often limited to single-center and single-task scenarios, making it difficult to generalize their results. To address this, we present a multi-center, multi-task labeled dataset. In this study, our dataset comprises three datasets obtained from different hospitals. The first set has 4940 panoramic radiography images and corresponding labels from the Stemmatological Hospital of the General Hospital of Ningxia Medical University. The second set includes 716 panoramic radiography images and labels from the People's Hospital of Yinchuan City, Ningxia. The third dataset contains 880 panoramic radiography images and labels from a hospital in Shenzhen, Guangdong Province. This comprehensive dataset encompasses three types of dental diseases: impacted teeth, periodontitis, and dental caries. Specifically, it comprises 2555 images related to impacted teeth, 2735 images related to periodontitis, and 1246 images related to dental caries. In order to evaluate the performance of the dataset, we conducted benchmark tests for segmentation and classification tasks on our dataset. The results show that the presented dataset could be effectively used for benchmarking segmentation and classification tasks critical to the diagnosis of dental diseases. To request our multi-center dataset, please visit the address: https://github.com/qinxin99/qinxini .

5.
Int J Biol Macromol ; 261(Pt 2): 129812, 2024 Feb 01.
Artigo em Inglês | MEDLINE | ID: mdl-38302033

RESUMO

The hypoglycemic effects of two recrystallized resistant starches, A-type (ARS) and B-type (BRS), were investigated in type 2 diabetic mice. Mice were treated with low-, medium-, or high-dose ARS, high-dose BRS, or high-dose ARS combined with BRS (ABRS). After 10 weeks of continuous intervention, the medium-dose ARS group showed a significant reduction in fasting blood glucose, area under the curve of glucose, triglyceride (P < 0.01), and low-density lipoprotein (P < 0.05) levels compared to the model group and an increase in high-density lipoprotein levels (P < 0.01). The peptide YY and glucagon-like peptide-1 levels in the high-dose ARS, BRS, and ABRS groups and the butyric acid yield in the medium-dose ARS and BRS groups were significantly increased (P < 0.01) compared to those in the model group. Medium- and high-dose ARS intervention efficiently increased the relative abundance of beneficial Bacteroidetes, Lactobacillus, Lachnospiraceae_NK4A136_group, and Faecalibaculum, and lowered the ratio of Firmicutes to Bacteroidetes. Overall, ARS exhibited greater advantages than BRS in lowering blood sugar levels.

6.
Heliyon ; 10(2): e24851, 2024 Jan 30.
Artigo em Inglês | MEDLINE | ID: mdl-38312592

RESUMO

Eucommia ulmoides Oliv. is an ancient and precious plant that has been used as medicine in China for more than 2000 years. Because its bark, leaves, seeds, and male flowers can be used in medicine, it plays an important role in medicine, food, chemical industry, and other fields, so it is also called "plant gold". 246 compounds have been isolated from E. ulmoides, which endow E. ulmoides with many unique pharmacological effects and make it wide to study in the fields of osteoporosis, hypertension, liver protection, and so on. Besides, E. ulmoides also has significant medicinal effects on anti-inflammatory, antioxidant, immunomodulation, and neuroprotection, and is often used in clinical compound medicines of traditional Chinese medicine. In addition to updating its ethnobotany, phytochemistry, pharmacology, and toxicology information, the economic botany of leaves, seeds, and male flowers was also introduced. It hopes hoping to fully understand this economically important Chinese medicine and provide a scientific basis for further development and utilization of E. ulmoides.

7.
Heliyon ; 10(2): e24649, 2024 Jan 30.
Artigo em Inglês | MEDLINE | ID: mdl-38298625

RESUMO

Background: In the pursuit of causal insights into neural circuit functionality, various interventions, including electrical, genetic, and pharmacological approaches, have been applied over recent decades. This study employs a comprehensive bibliometric perspective to explore the field of neural circuits. Methods: Reviews and articles on neural circuits were obtained from the Web of Science Core Collection (WOSCC) database on Apr. 12, 2023. In this article, co-authorship analysis, co-occurrence analysis, citation analysis, bibliographic analysis, and co-citation analysis were used to clarify the authors, journals, institutions, countries, topics, and internal associations between them. Results: More than 2000 organizations from 52 different countries published 3975 articles in the field of "neural circuit" were used to analysis. Luo liqun emerged as the most prolific author, and Deisseroth Karl garners the highest co-citations (3643). The Journal of Neuroscience leaded in publications, while Nature toped in citations. Chinese Academy of Science recorded the highest article count institutionally, with Stanford University ranking first with 14,350 citations. Since 2020, neurodynamic, anxiety-related mechanisms, and GABAergic neurons have gained prominence, shaping the trajectory of neural circuitry research. Conclusions: Our investigation has discerned a paradigmatic reorientation towards neurodynamic processes, anxiety-related mechanisms, and GABAergic neurons within the domain of neural circuit research. This identification intimates a prospective trajectory for the field. In the future, it is imperative for research endeavors to accord priority to the translational application of these discernments, with the aim of materializing tangible clinical solutions.

8.
Heliyon ; 10(2): e24378, 2024 Jan 30.
Artigo em Inglês | MEDLINE | ID: mdl-38298673

RESUMO

Background: Epidermal growth factor receptor (EGFR) mutations have been identified as promising therapeutic targets for non-small cell lung cancer. Osimertinib, a third-generation EGFR-tyrosine kinase inhibitor-targeting drug, has good anti-tumor ability and excellent intracranial effects. However, management of osimertinib resistance is a clinical challenge. The clinical benefit of osimertinib combined with the antiangiogenic drug, bevacizumab, remains to be determined. Case presentation: A 40-year-old female with right lung adenocarcinoma (cT2aN3M1c, IVb) was confirmed positive for EGFR exon 19 deletion mutation (c.2235_2249del, 1.3%). After receiving 5 months of osimertinib (80 mg, qd) therapy, the patient's disease progressed and she subsequently accepted treatment with osimertinib (80 mg, qd) plus bevacizumab (15 mg/kg, q21d) and achieved notable clinical remission for 23 months until renal impairment occurred, after which bevacizumab was discontinued. The patient had 6 months of remission before progression, after which bevacizumab was added again. To date, the disease has been under control. The brain lesion showed partial response again, and the side effects of bevacizumab were tolerable. The overall survival time exceeded 4 years. Conclusion: This case report describes a treatment strategy for osimertinib-resistant patients with EGFR exon 19 deletion mutations. Metronomic treatment with osimertinib plus bevacizumab was achieved for more than 4 years.

9.
Plant Cell ; 2024 Jan 31.
Artigo em Inglês | MEDLINE | ID: mdl-38299379

RESUMO

The flower-infecting fungus Ustilaginoidea virens causes rice false smut, which is a severe emerging disease threatening rice (Oryza sativa) production worldwide. False smut not only reduces yield, but more importantly produces toxins on grains, posing a great threat to food safety. U. virens invades spikelets via the gap between the two bracts (lemma and palea) enclosing the floret and specifically infects the stamen and pistil. Molecular mechanisms for the U. virens-rice interaction are largely unknown. Here, we demonstrate that rice flowers predominantly employ chitin-triggered immunity against U. virens in the lemma and palea, rather than in the stamen and pistil. We identify a crucial U. virens virulence factor, named UvGH18.1, which carries glycoside hydrolase activity. Mechanistically, UvGH18.1 functions by binding to and hydrolyzing immune elicitor chitin and interacting with the chitin receptor CHITIN ELICITOR BINDING PROTEIN (OsCEBiP) and co-receptor CHITIN ELICITOR RECEPTOR KINASE1 (OsCERK1) to impair their chitin-induced dimerization, suppressing host immunity exerted at the lemma and palea for gaining access to the stamen and pistil. Conversely, pretreatment on spikelets with chitin induces a defense response in the lemma and palea, promoting resistance against U. virens. Collectively, our data uncover a mechanism for a U. virens virulence factor and the critical location of the host-pathogen interaction in flowers and provide a potential strategy to control rice false smut disease.

11.
Plant Cell Environ ; 2024 Feb 05.
Artigo em Inglês | MEDLINE | ID: mdl-38314665

RESUMO

As the most abundant form of methylation modification in messenger RNA (mRNA), the distribution of N6 -methyladenosine (m6 A) has been preliminarily revealed in herbaceous plants under salt stress, but its function and mechanism in woody plants were still unknown. Here, we showed that global m6 A levels increased during poplar response to salt stress. Methylated RNA immunoprecipitation sequencing (MeRIP-seq) revealed that m6 A significantly enriched in the coding sequence region and 3'-untranslated regions in poplar, by recognising the conserved motifs, AGACU, GGACA and UGUAG. A large number of differential m6 A transcripts have been identified, and some have been proved involving in salt response and plant growth and development. Further combined analysis of MeRIP-seq and RNA-seq revealed that the m6 A hypermethylated and enrich in the CDS region preferred to positively regulate expression abundance. Writer inhibitor, 3-deazaneplanocin A treatment increased the sensitivity of poplar to salt stress by reducing mRNA stability to regulate the expression of salt-responsive transcripts PagMYB48, PagGT2, PagNAC2, PagGPX8 and PagARF2. Furthermore, we verified that the methyltransferase PagFIP37 plays a positively role in the response of poplar to salt stress, overexpressed lines have stronger salt tolerance, while RNAi lines were more sensitive to salt, which relied on regulating mRNA stability in an m6 A manner of salt-responsive transcripts PagMYB48, PagGT2, PagNAC2, PagGPX8 and PagARF2. Collectively, these results revealed the regulatory role of m6 A methylation in poplar response to salt stress, and revealed the importance and mechanism of m6 A methylation in the response of woody plants to salt stress for the first time.

12.
Immunol Invest ; : 1-13, 2024 Feb 05.
Artigo em Inglês | MEDLINE | ID: mdl-38314676

RESUMO

Cancer is an abnormal proliferation of cells that is stimulated by cyclin-dependent kinases (CDKs) and defective cell cycle regulation. The essential agent that drive the cell cycle, CDK4/6, would be activated by proliferative signals. Activated CDK4/6 results in the phosphorylation of the neuroblastoma protein (RB) and the release of the transcription factor E2F, which promotes the cell cycle progression. CDK4/6 inhibitor (CDK4/6i) has been currently a research focus, which inhibits the CDK4/6-RB-E2F axis, thereby reducing the cell cycle transition from G1 to S phase and mediating the cell cycle arrest. This action helps achieve an anti-tumor effect. Recent research has demonstrated that CDK4/6i, in addition to contributing to cell cycle arrest, is also essential for the interaction between the tumor cells and the host immune system, i.e., activating the immune system, strengthening the tumor antigen presentation, and reducing the number of regulatory T cells (Treg). Additionally, CDK4/6i would elevate the level of PD-L1, an immunosuppressive factor, in tumor cells, and CDK4/6i in combination with anti-PD-L1 therapy would more effectively reduce the tumor growth. Our results showed that CDK4/6i caused autophagy and senescence in tumor cells. Herein, the impact of CDK4/6i on the immune microenvironment of malignant tumors was mainly focused, as well as their interaction with immune checkpoint inhibitors in affecting anti-tumor immunity.

13.
ACS Synth Biol ; 2024 Feb 10.
Artigo em Inglês | MEDLINE | ID: mdl-38340070

RESUMO

Serratia marcescens has garnered increasing attention as a promising host for valuable compound production. However, the lack of an efficient gene regulation toolkit severely hampers its applications. Here, a library of stationary phase promoters was screened in S. marcescens HBA7 using RNA-seq and RT-qPCR, revealing a 43-fold regulatory range with the red fluorescent protein mKate2 as the reporter. The ß-galactosidase was employed to demonstrate the universality in driving the expression of different proteins. The wide-ranging utility of these promoters in different hosts was demonstrated in Escherichia coli. Moreover, to assess their potential application, the strongest promoter, P2, was employed to express the swrW gene, resulting in a roughly 20-fold increase in serrawettin W1 production in S. marcescens HBQA7ΔswrW. In summary, this study successfully constructed a gradient-strength stationary phase promoter library, providing an effective toolkit for gene regulation and secondary metabolite production in diverse prokaryotes, including S. marcescens and E. coli.

14.
Dig Liver Dis ; 2024 Feb 09.
Artigo em Inglês | MEDLINE | ID: mdl-38341376
15.
Food Chem ; 445: 138648, 2024 Feb 03.
Artigo em Inglês | MEDLINE | ID: mdl-38354639

RESUMO

This research investigates the formation of amyloid fibrils using enzymatically hydrolyzed peptides from gluten, including its components glutenin and gliadin. After completing the fibrillation incubation, the gluten group demonstrated the most significant average particle size (908.67 nm) and conversion ratio (57.64 %), with a 19.21 % increase in thioflavin T fluorescence intensity due to self-assembly. The results indicated increased levels of ß-sheet structures after fibrillation. The gliadin group exhibited the highest zeta potential (∼13 mV) and surface hydrophobicity (H0 = 809.70). Around 71.15 % of predicted amyloidogenic regions within gliadin peptides showed heightened hydrophobicity. These findings emphasize the collaborative influence of both glutenin and gliadin in the formation of gluten fibrils, influenced by hydrogen bonding, hydrophobic, and electrostatic interactions. They also highlight the crucial role played by gliadin with amyloidogenic fragments such as ILQQIL and SLVLQTL, aiming to provide a theoretical basis for understanding the utilization of gluten proteins.

16.
Mol Nutr Food Res ; : e2200771, 2024 Feb 14.
Artigo em Inglês | MEDLINE | ID: mdl-38356045

RESUMO

SCOPE: Early diabetic retinopathy (DR) is characterized by chronic inflammation, excessive oxidative stress, and retinal microvascular damage. Syringaresinol (SYR), as a natural polyphenolic compound, has been proved to inhibit many disease progression due to its antiinflammatory and antioxidant properties. The present study focuses on exploring the effect of SYR on hyperglycemia-induced early DR as well as the underlying mechanisms. METHODS AND RESULTS: Wild-type (WT) and nuclear factor erythroid 2-related factor 2 (Nrf2)-knockout C57BL/6 mice of type 1 diabetes and high glucose (HG)-induced RF/6A cells are used as in vivo and in vitro models, respectively. This study finds that SYR protects the retinal structure and function in diabetic mice and reduces the permeability and apoptosis of HG-treated RF/6A cells. Meanwhile, SYR distinctly mitigates inflammation and oxidative stress in vivo and vitro. The retinal microvascular damages are suppressed by SYR via downregulating hypoxia-inducible factor-1α (HIF-1α)/vascular endothelial growth factor (VEGF) pathway. Whereas, SYR-provided protective effects are diminished in Nrf2-knockout mice, indicating that SYR improves DR progression by activating Nrf2. Similarly, SYR cannot exert protective effects against HG-induced oxidative stress and endothelial injury in small interfering RNA (siRNA)-Nrf2-transfected RF/6A cells. CONCLUSION: In summary, SYR suppresses oxidative stress via activating Nrf2 antioxidant pathway, which ameliorates retinal microvascular damage by downregulating HIF-1α/VEGF, thereby alleviating early DR progression.

17.
Nurs Crit Care ; 2024 Feb 15.
Artigo em Inglês | MEDLINE | ID: mdl-38358027

RESUMO

BACKGROUND: Although the circuit condensate, an ideal bacterial reservoir during mechanical ventilation, may flow into the humidifier reservoir, no studies have investigated if humidifier reservoir colonized bacteria colonize other circuit locations with airflow. AIMS: We aimed to prove whether the humidifier reservoir colonized bacteria colonize other circuit locations with airflow and provide some advice on the disposal of condensate in the clinical setting. STUDY DESIGN: An in vitro experiment was conducted. Mechanical ventilation simulators (n = 90) were divided into sterile water group (n = 30) and broth group (n = 60). In the sterile water group, sterile water was used for humidification, either Acinetobacter baumannii or Pseudomonas aeruginosa were inoculated to humidifier water in the humidifier reservoir, each accounted for 50% of the simulators. The broth group was performed the same as the sterile water group except for the addition of broth into the humidified water. After 24, 72, and 168 h of continuous ventilation, the humidifier water and different locations of the circuits were sampled for bacterial culture. RESULTS: All bacterial culture results of the sterile water group were negative. Bacteria in the humidifier water continued to proliferate in the broth group. With prolonged ventilation, the bacteria at the humidifier reservoir outlet increased. The bacteria at the humidifier reservoir outlet were much more in the Pseudomonas aeruginosa subgroup than in the Acinetobacter baumannii subgroup and the difference was statistically significant (p < .05). During continuous ventilation, no bacterial growth occurred at 10 cm from the humidifier reservoir outlet and the Y-piece of the ventilator circuits. CONCLUSIONS: Sterile water in the humidifier reservoir was not conducive to bacterial growth. Even if bacteria grew in the humidifier reservoir and could reach the humidifier reservoir outlet, colonization of further circuit locations with the airflow was unlikely. During a certain mechanical ventilation time, the amount of bacteria reaching the outlet of the humidifier reservoir varied due to different mobility of bacteria. RELEVANCE TO CLINICAL PRACTICE: In a clinical setting, nurses should not worry about a small amount of condensate backflow into the humidifier reservoir. Draining condensate into the humidifier reservoir can be used as a low risk and convenient method in clinical practice.

19.
Artigo em Inglês | MEDLINE | ID: mdl-38350161

RESUMO

PURPOSE: To explore the influence of preoperative factors, including varying pupil sizes and refractive attributes, on postoperative disability glare in patients undergoing Implantable Collamer Lens (ICL) implantation. SETTING: Second Affiliated Hospital, Nanchang University. DESIGN: Prospective observational study. METHODS: We analyzed the preoperative ocular characteristics and six-month postoperative glare status in eligible patients who underwent EVO-Visian ICL V4c (VICMO) implantation. The disability glare criteria encompassed a glare symptom score >6 and glare sensitivity exceeding 1:2.7. Logistic regression analysis was used to explore the relationship between the preoperative ocular parameters and post-ICL glare. RESULTS: The study included 95 patients (mean age, 26.04 ± 6.29 years), comprising 30 males (58 eyes) and 65 females (129 eyes). Multivariate analysis revealed a significant correlation between postoperative disability glare and increased spherical power in preoperative mesopic pupils (ß = -0.124, p = 0.039), as well as elevated cylinder power in preoperative mesopic (ß = -0.412, p = 0.009) and photopic pupils (ß = -0.430, p = 0.007). Moreover, a larger preoperative mesopic pupil diameter (ß = 0.561, p = 0.005) demonstrated a significant correlation with disability glare. CONCLUSIONS: Preoperative mesopic pupil dimensions and associated refractive parameters, such as sphere and cylinder were correlated with disability glare, including the cylinder aspect in photopic pupils, which can assist clinicians in optimizing preoperative selection for ICL implantation, aiding in the anticipation of potential disability glare risks.

20.
Angew Chem Int Ed Engl ; : e202319758, 2024 Feb 14.
Artigo em Inglês | MEDLINE | ID: mdl-38353649

RESUMO

Fluorinated small molecules are commonly utilized in the realm of functional small-molecule chemistry, and N-difluoromethyl (N-CF2H) compounds are especially fascinating because of their unique and unexplored physiochemical properties. However, despite limited progress, a general applicable methodological approach to the synthesis of N-CF2H compounds remains elusive. Herein, guided by computation, we present an operationally simple and practical protocol to access N-CF2H amides and related carbonyl derivatives. The protocol utilizes a one-pot conversion of thioformamides via desulfurization-fluorination and acylation, providing N-difluoromethylcarbamoyl fluoride building blocks that can be further diversified to a diversity of unexplored N-CF2H carbonyl compounds with rich functionality. Furthermore, preliminary studies on their properties and stability showcased their application in pharmaceuticals and agrochemicals.

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