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Synthesis and antibacterial evaluation of novel 1,2,4-oxadiazole derivatives bearing a 1,3,4-oxadiazole thioether moiety 含有1,3,4-恶二唑硫醚片段的新型1,2,4-恶二唑衍生物的合成及抗菌评价
IF 1.6 4区 化学 Q4 CHEMISTRY, INORGANIC & NUCLEAR Pub Date : 2026-06-03 Epub Date: 2026-03-24 DOI: 10.1080/10426507.2026.2647299
Yong Liu (Data curation Writing – original draft) , Lei Shao (Writing – original draft) , Huanhuan Liu (Data curation) , Xin Dai (Writing – original draft) , Chenghao Tang (Writing – review & editing)
A series of novel 1,2,4-oxadiazole derivatives incorporating 1,3,4-oxadiazole thioether moiety were designed and synthesized, and their in vitro antibacterial activities against Xanthomonas oryzae pv. oryzae (Xoo), Pseudomonas syringae pv. actinidiae (Psa), and Xanthomonas axonopodis pv. citri (Xac) were evaluated. Bioassay results revealed that compounds 6b, 6r, and 6s showed excellent inhibitory effects against Psa, compounds 6r and 6s indicated pronounced inhibitory activity against Xoo, compounds 6b and 6r demonstrated notable inhibitory activity against Xac. Future work will focus on exploring their bioactive potential, with the aim of discovering novel 1,2,4-oxadiazole derivatives and evaluating their broader applicability.
设计合成了一系列含有1,3,4-恶二唑硫醚基团的新型1,2,4-恶二唑衍生物,并对其体外抑菌活性进行了研究。oryzae (Xoo), syringae假单胞菌pv。actinidiae (Psa)和Xanthomonas axonopodis pv。柠檬酸(Xac)进行评价。生物实验结果表明,化合物6b、6r和6s对Psa具有良好的抑制作用,化合物6r和6s对Xoo具有明显的抑制活性,化合物6b和6r对Xac具有显著的抑制活性。未来的工作将集中于探索它们的生物活性潜力,目的是发现新的1,2,4-恶二唑衍生物并评估其更广泛的适用性。
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引用次数: 0
Influence of biochar and zeolite-based Zn and Fe nano composites on nutrient content, uptake, and agronomic fortification of Zn and Fe in rice 生物炭和沸石基锌铁纳米复合材料对水稻锌铁营养含量、吸收和农艺强化的影响
IF 1.6 4区 化学 Q4 CHEMISTRY, INORGANIC & NUCLEAR Pub Date : 2026-06-03 Epub Date: 2026-03-01 DOI: 10.1080/10426507.2026.2640178
D. Arul Raja Sekaran (Formal analysis Funding acquisition Investigation Resources) , M Bakkiyaraj (Conceptualization Data curation) , P. Rajakrishnamoorthy (Methodology Validation Visualization Writing – original draft) , R Singaravel (Supervision Writing – review & editing)
The present investigation aims to optimize the effect of biochar and zeolite-based nano composites (Zn and Fe) on the various factors such as nutrient content and nutrient uptake and Agronomic fortification of Zn and Fe in rice. Seven types of completely randomized design treatment were examined using Aduthurai-43 rice (ADT 43) with three replications, namely, Tr-1 – RFD NPK(120:40:40) (Control), Tr-2 – RFD + FeSO4 at 25 kg·ha−1 + ZnSO4 at 25 kg·ha−1, Tr-3 – RFD + nano FeO + nano ZnO foliar at 500 ppm, Tr-4 – RFD + 1 g·kg−1 of nano zeolite composite, Tr-5 – RFD + 1 g·kg−1 of nano biochar composite, Tr-6 – RFD + nano FeO + nano ZnO foliar each at 500 ppm + nano zeolite composite, and Tr-7 – RFD + nano FeO + nano ZnO foliar each at 500 ppm + 1 g·kg−1 nano biochar composite. To determine the major and micro nutrient contents, grain samples and straw samples (harvest) were collected and examined using two acid extract, prepared from H2SO4 and HClO4 solution with 5:1 ratio. Among the treatments, Tr-7 significantly increased the NPK content of 0.99, 0.30 and 0.69 and Zn and Fe content by registering 22.4 and 246 mg·kg−1 of Zn and Fe, respectively, by grain and 50.7 and 241 mg·kg−1, respectively, by straw.
本研究旨在优化生物炭和沸石基纳米复合材料(Zn和Fe)对水稻养分含量、养分吸收和锌铁农艺强化等各因素的影响。七种类型的完全随机法治疗检查使用Aduthurai-43大米(ADT 43)三个复制,即Tr-1——RFD氮磷钾(120:40:40)(控制),Tr-2 - RFD +摘要在25公斤·哈在25公斤−1 + ZnSO4·哈−1,Tr-3 - RFD +纳米FeO说+纳米氧化锌叶面在500 ppm, Tr-4 - RFD + 1 g·公斤−1纳米沸石复合,Tr-5 - RFD + 1 g·公斤−1纳米生物炭复合,Tr-6 - RFD +纳米FeO说+纳米氧化锌叶面每个在500 ppm +纳米沸石复合,和Tr-7 - RFD +纳米FeO +纳米ZnO叶面各为500 ppm + 1 g·kg−1纳米生物炭复合材料。采集谷物样品和秸秆样品(收获),采用H2SO4和HClO4溶液以5:1的比例配制两种酸提取物,测定主要和微量营养素含量。其中,Tr-7处理显著提高了氮磷钾含量0.99、0.30和0.69,籽粒Zn和Fe含量分别为22.4和246 mg·kg - 1,秸秆Zn和Fe含量分别为50.7和241 mg·kg - 1。
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引用次数: 0
Research progress of the synthesis of phosphorothioates, phosphonothioates and phosphinothioates 硫代磷、硫代磷和硫代磷的合成研究进展
IF 1.6 4区 化学 Q4 CHEMISTRY, INORGANIC & NUCLEAR Pub Date : 2026-06-03 Epub Date: 2026-03-17 DOI: 10.1080/10426507.2026.2647298
Xiaosong Wang (Writing – original draft) , Li Ye (Writing – original draft) , Qiaoyu Gan (Supervision) , Tingting Zhang (Resources Supervision) , Lixin Ma (Supervision Visualization Writing – original draft) , Yingli Liu (Supervision Writing – original draft) , Xi Chen (Supervision Writing – review & editing) , Zeqi Jiang (Supervision Writing – review & editing)
Phosphorothioates, phosphonothioates and phosphinothioates constitute an important class of compounds that have been widely applied in the fields of pesticides, pharmaceuticals, and organic synthesis. In this review, the synthesis of phosphorothioate, phosphonothioate and phosphinothioate are classified into two categories according to their catalytic modes, including metal catalysis, halogen activation, base catalysis, photocatalysis, electrocatalysis, and organocatalysis. The representative advances in the synthesis of this compounds reported up to 2026 are comprehensively summarized.
硫代磷、硫代磷和硫代磷是一类重要的化合物,在农药、医药、有机合成等领域有着广泛的应用。本文根据硫代磷、硫代磷和硫代磷的催化方式,将其合成分为金属催化、卤素活化、碱催化、光催化、电催化和有机催化两大类。全面综述了截至2026年这类化合物的代表性合成进展。
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引用次数: 0
Investigation of cooperativity in triple adducts of phosphangulene PG(HX)(Y)–: a theoretical study 磷酸二烯三加合物PG(HX)(Y) -协同性的理论研究
IF 1.6 4区 化学 Q4 CHEMISTRY, INORGANIC & NUCLEAR Pub Date : 2026-06-03 Epub Date: 2026-02-18 DOI: 10.1080/10426507.2026.2632949
Abdul Bari Omary (Formal analysis Investigation) , Abedien Zabaradsti (Formal analysis Investigation Writing – review & editing)
A theoretical study of the model dyad and triad complexes of general formula PG(HX), PG(Y) and PG(HX)(Y) (HX = HF, HCl and Y = F, Cl, C≡N, N≡C) has been carried out using density functional theory at B3LYP/6-311++G(2d,2p) computational level and basis set. Four distinctive non-covalent interaction patterns, including pnictogen bond (PnB), tetrel bond (TtB), chalcogen bond (ChB), and hydrogen bond (HB), were found for complex formation between phosphangulene (PG) with CN, NC, F, Cl anions and HF, HCl neutral molecules. Each HX and Y component can interact on the apex or at basal sites of the PG molecule and result in PG(HX)a(Y)b or PG(Y)a(HX)b aggregates. From the anticipated models, stabilities of the PG(CN)a(HF)b, PG(NC)a(HF)b, PG(F)a(HF)b, PG(F)a(HF)b, and PG(Cl)a(HF)b triads are greater than other types. The electron release of PG to the HX molecules helps it to take electron from Y ions, thus PG(HX)(Y) triads show greater stability and considerable cooperative effect relative to corresponding dyad adducts. Natural bond orbital theory (NBO) and Bader’s theory of “atoms in molecules” (AIM) methods have been applied to analyze the intermolecular interactions. Strong correlations have been observed between stabilities and charge transfer (qCT) in the analyzed systems.
利用密度泛函理论,在B3LYP/6-311++G(2d,2p)计算水平和基集上对通式PG(HX), PG(Y)−和PG(HX)(Y)−(HX = HF, HCl和Y = F−,Cl−,C≡N−,N≡C−)的模型二元和三元配合物进行了理论研究。在磷烯(PG)与CN−、NC−、F−、Cl−阴离子和HF、HCl中性分子之间形成络合物时,发现了四种不同的非共价相互作用模式,包括PnB键、TtB键、ChB键和HB键。每种HX和Y组分可以在PG分子的顶端或基部相互作用,导致PG(HX)a(Y)b−或PG(Y)a(HX)b−聚集。从预期的模型来看,PG(CN)a(HF)b−、PG(NC)a(HF)b−、PG(F)a(HF)b−、PG(F)a(HF)b−和PG(Cl)a(HF)b−的稳定性比其他类型的三联体要好。PG向HX分子的电子释放有助于其从Y离子中获取电子,因此PG(HX)(Y)−三合体相对于相应的二合体加合物表现出更大的稳定性和可观的协同效应。应用自然键轨道理论(NBO)和Bader的“分子中原子”理论(AIM)方法分析了分子间相互作用。在所分析的体系中,稳定性与电荷转移(qCT)之间存在很强的相关性。
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引用次数: 0
Design, synthesis, pharmacological evaluation and in-silico analysis of quinazoline derivatives as potential therapeutic agents 喹唑啉衍生物作为潜在治疗剂的设计、合成、药理学评价和计算机分析
IF 1.6 4区 化学 Q4 CHEMISTRY, INORGANIC & NUCLEAR Pub Date : 2026-06-03 Epub Date: 2026-03-09 DOI: 10.1080/10426507.2026.2642861
Kholoud Zaki (Data curation Formal analysis Investigation Methodology) , Zeinab K. Hamza (Conceptualization Data curation Formal analysis Investigation Methodology) , Adel A. H. Abdel-Rahman (Conceptualization Funding acquisition Project administration Resources Supervision Writing – original draft) , Magdy M. Hemdan (Conceptualization Funding acquisition Project administration Writing – original draft) , Ibrahim F. Nassar (Formal analysis Project administration Software Supervision Writing – original draft) , Ahmed F. El-Sayed (Investigation Software Visualization Writing – original draft) , Mosaad A. Abdel-Wahhab (Conceptualization Data curation Project administration Supervision Validation Writing – review & editing)
This study focuses on the design, synthesis, and comprehensive biological evaluation of novel quinazoline derivatives as potential therapeutic agents. The structures of nine synthesized compounds were confirmed using spectral methods such as infrared (IR), proton nuclear magnetic resonance (1H NMR) spectroscopy, and elemental analysis. These compounds were assessed for antimicrobial, antioxidant, and anticancer activities against human cancer cell lines including hepatocellular carcinoma (HepG-2), breast cancer (MCF-7), and colorectal carcinoma (HCT-116). Among them, Compounds 8 and 9 exhibited remarkable biological activities. Both compounds demonstrated significant antimicrobial and antioxidant effects, alongside potent antiproliferative activity against (HepG-2), breast cancer (MCF-7) and colorectal carcinoma (HCT-116) cell lines. Notably, Compound 8 showed superior cytotoxicity with IC50 values of 30.81, 53.41, and 76.73 µM against HepG-2, MCF-7, and HCT-116 cells, respectively, outperforming Compound 9. Molecular docking studies corroborated these results, revealing strong binding affinities of Compounds 8 and 9 to key protein targets implicated in antimicrobial and anticancer mechanisms, including Escherichia coli DNA gyrase, Staphylococcus aureus dihydropteroate synthase (DHPS), CDK2 and EGFR. Furthermore, in-silico ADMET predictions indicated favorable drug-likeness and low toxicity risks, aligning with Pfizer’s drug design guidelines. Overall, Compounds 8 and 9 emerge as promising leads with broad-spectrum therapeutic potential for pharmaceutical and food industry applications.
本研究的重点是新型喹唑啉衍生物的设计、合成和综合生物学评价作为潜在的治疗剂。9个合成化合物的结构通过红外(IR)、质子核磁共振(1H NMR)谱和元素分析等光谱方法得到了证实。这些化合物对人类肝癌(HepG-2)、乳腺癌(MCF-7)和结直肠癌(HCT-116)的抗菌、抗氧化和抗癌活性进行了评估。其中化合物8和9表现出显著的生物活性。这两种化合物均显示出显著的抗菌和抗氧化作用,并具有对HepG-2、乳腺癌(MCF-7)和结直肠癌(HCT-116)细胞系的有效抗增殖活性。值得注意的是,化合物8对HepG-2、MCF-7和HCT-116细胞的IC50值分别为30.81、53.41和76.73µM,优于化合物9。分子对接研究证实了这些结果,揭示了化合物8和9与抗菌和抗癌机制相关的关键蛋白靶点具有很强的结合亲和力,包括大肠杆菌DNA旋切酶、金黄色葡萄球菌二氢蝶酸合成酶(DHPS)、CDK2和EGFR。此外,计算机ADMET预测显示良好的药物相似性和低毒性风险,符合辉瑞的药物设计指南。综上所述,化合物8和9在制药和食品工业中具有广泛的治疗潜力。
{"title":"Design, synthesis, pharmacological evaluation and in-silico analysis of quinazoline derivatives as potential therapeutic agents","authors":"Kholoud Zaki (Data curation Formal analysis Investigation Methodology) ,&nbsp;Zeinab K. Hamza (Conceptualization Data curation Formal analysis Investigation Methodology) ,&nbsp;Adel A. H. Abdel-Rahman (Conceptualization Funding acquisition Project administration Resources Supervision Writing – original draft) ,&nbsp;Magdy M. Hemdan (Conceptualization Funding acquisition Project administration Writing – original draft) ,&nbsp;Ibrahim F. Nassar (Formal analysis Project administration Software Supervision Writing – original draft) ,&nbsp;Ahmed F. El-Sayed (Investigation Software Visualization Writing – original draft) ,&nbsp;Mosaad A. Abdel-Wahhab (Conceptualization Data curation Project administration Supervision Validation Writing – review & editing)","doi":"10.1080/10426507.2026.2642861","DOIUrl":"10.1080/10426507.2026.2642861","url":null,"abstract":"<div><div>This study focuses on the design, synthesis, and comprehensive biological evaluation of novel quinazoline derivatives as potential therapeutic agents. The structures of nine synthesized compounds were confirmed using spectral methods such as infrared (IR), proton nuclear magnetic resonance (<sup>1</sup>H NMR) spectroscopy, and elemental analysis. These compounds were assessed for antimicrobial, antioxidant, and anticancer activities against human cancer cell lines including hepatocellular carcinoma (HepG-2), breast cancer (MCF-7), and colorectal carcinoma (HCT-116). Among them, Compounds <strong>8</strong> and <strong>9</strong> exhibited remarkable biological activities. Both compounds demonstrated significant antimicrobial and antioxidant effects, alongside potent antiproliferative activity against (HepG-2), breast cancer (MCF-7) and colorectal carcinoma (HCT-116) cell lines. Notably, Compound <strong>8</strong> showed superior cytotoxicity with IC<sub>50</sub> values of 30.81, 53.41, and 76.73 µM against HepG-2, MCF-7, and HCT-116 cells, respectively, outperforming Compound <strong>9</strong>. Molecular docking studies corroborated these results, revealing strong binding affinities of Compounds <strong>8</strong> and <strong>9</strong> to key protein targets implicated in antimicrobial and anticancer mechanisms, including <em>Escherichia coli</em> DNA gyrase, <em>Staphylococcus aureus</em> dihydropteroate synthase (DHPS), CDK2 and EGFR. Furthermore, <em>in-silico</em> ADMET predictions indicated favorable drug-likeness and low toxicity risks, aligning with Pfizer’s drug design guidelines. Overall, Compounds <strong>8</strong> and <strong>9</strong> emerge as promising leads with broad-spectrum therapeutic potential for pharmaceutical and food industry applications.</div></div>","PeriodicalId":20056,"journal":{"name":"Phosphorus, Sulfur, and Silicon and the Related Elements","volume":"201 6","pages":"Pages 957-979"},"PeriodicalIF":1.6,"publicationDate":"2026-06-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148207929","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Discovery of novel antibiotic thioether derivatives against tobacco bacterial wilt (Ralstonia solanacearum) 新型抗烟草青枯病抗生素硫醚衍生物的发现
IF 1.6 4区 化学 Q4 CHEMISTRY, INORGANIC & NUCLEAR Pub Date : 2026-06-03 Epub Date: 2026-02-28 DOI: 10.1080/10426507.2026.2636154
Jiting Li (Investigation Resources Writing – original draft) , Feng Hao (Conceptualization Formal analysis Methodology Resources Software Visualization) , Zhihua Liu (Methodology) , Xinhui Wang (Resources) , Ran Song (Formal analysis) , Yimai Yin (Resources) , Wei Jiang (Software) , Xiaoxi Si (Software) , Wenjin Sun (Data curation) , Le Cai (Project administration Supervision) , Fengmei Zhang (Funding acquisition Project administration)
This study focuses on the synthesis of six novel thioether derivatives with potent antimicrobial activity against Ralstonia solanacearum, the causative agent of tobacco bacterial wilt. This disease, which has caused significant economic losses, has become increasingly resistant to traditional bactericides. In response, the study investigates the potential of thioether derivatives, known for their broad spectrum of biological activities, as eco-friendly alternatives. Through SEM observations, molecular docking, and DFT calculations, we identified DHFR as a potential target for these compounds, particularly highlighting compound R4, which showed superior activity compared to conventional controls. Additionally, toxicity predictions and ADME simulations suggest that compound R4 could be a promising, safe agricultural antimicrobial agent. This research aims to expand the range of agricultural chemical frameworks and contribute to the development of more effective and environmentally friendly solutions for pest and disease control.
本研究合成了6种新型硫醚衍生物,并对烟草青枯病病原菌茄枯菌(Ralstonia solanacearum)具有较强的抗菌活性。这种造成重大经济损失的疾病对传统杀菌剂的抗药性越来越强。作为回应,该研究调查了硫醚衍生物作为环保替代品的潜力,硫醚衍生物以其广泛的生物活性而闻名。通过扫描电镜观察、分子对接和DFT计算,我们确定DHFR是这些化合物的潜在靶标,特别是化合物R4,与常规对照相比,它表现出更强的活性。此外,毒性预测和ADME模拟表明,化合物R4可能是一种有前途的、安全的农业抗菌剂。这项研究的目的是扩大农业化学框架的范围,并有助于制定更有效和环境友好的病虫害控制解决方案。
{"title":"Discovery of novel antibiotic thioether derivatives against tobacco bacterial wilt (Ralstonia solanacearum)","authors":"Jiting Li (Investigation Resources Writing – original draft) ,&nbsp;Feng Hao (Conceptualization Formal analysis Methodology Resources Software Visualization) ,&nbsp;Zhihua Liu (Methodology) ,&nbsp;Xinhui Wang (Resources) ,&nbsp;Ran Song (Formal analysis) ,&nbsp;Yimai Yin (Resources) ,&nbsp;Wei Jiang (Software) ,&nbsp;Xiaoxi Si (Software) ,&nbsp;Wenjin Sun (Data curation) ,&nbsp;Le Cai (Project administration Supervision) ,&nbsp;Fengmei Zhang (Funding acquisition Project administration)","doi":"10.1080/10426507.2026.2636154","DOIUrl":"10.1080/10426507.2026.2636154","url":null,"abstract":"<div><div>This study focuses on the synthesis of six novel thioether derivatives with potent antimicrobial activity against <em>Ralstonia solanacearum</em>, the causative agent of tobacco bacterial wilt. This disease, which has caused significant economic losses, has become increasingly resistant to traditional bactericides. In response, the study investigates the potential of thioether derivatives, known for their broad spectrum of biological activities, as eco-friendly alternatives. Through SEM observations, molecular docking, and DFT calculations, we identified DHFR as a potential target for these compounds, particularly highlighting compound <strong>R4</strong>, which showed superior activity compared to conventional controls. Additionally, toxicity predictions and ADME simulations suggest that compound <strong>R4</strong> could be a promising, safe agricultural antimicrobial agent. This research aims to expand the range of agricultural chemical frameworks and contribute to the development of more effective and environmentally friendly solutions for pest and disease control.</div></div>","PeriodicalId":20056,"journal":{"name":"Phosphorus, Sulfur, and Silicon and the Related Elements","volume":"201 6","pages":"Pages 897-903"},"PeriodicalIF":1.6,"publicationDate":"2026-06-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148207932","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Quantum chemical engineering of end-capping acceptors on DNR based molecules for their efficient optoelectronic properties to enhance photovoltaic properties 基于DNR分子的末端封盖受体的量子化学工程,利用其高效的光电性能来增强光伏性能
IF 1.6 4区 化学 Q4 CHEMISTRY, INORGANIC & NUCLEAR Pub Date : 2026-06-03 Epub Date: 2026-03-04 DOI: 10.1080/10426507.2026.2640187
Mahnoor Awan (Conceptualization Data curation Writing – original draft) , Muhammad Muzammal (Formal analysis Methodology) , Hamza Saleem (Software Validation) , Muhammad Mohsin (Formal analysis Software Supervision Validation Visualization) , Muhammad Azam Qamar (Writing – review & editing)
To enhance the photovoltaic attributes of organic solar cells, six new molecules (A-D-A type) are tailored through end-capped modification of the existing DNO15T molecule. To evaluate their properties, various computational calculations have been performed using density functional theory (DFT) with B3LYP/6–31G(d,p) functional. We studied several geometrical attributes such as density of states (DOS), dipole moment, excitation and binding energy, open circuit voltage (VOC), fill factor, molecular electrostatic potential, alignment of frontier molecular orbitals, transition density matrix (TDM), reorganizational energy, molecular planarity, deviation of planarity of all the tailored molecules (DN1–DN6) along with the reference DNR. NCI graphs and isosurfaces were additionally employed to analyze their non-covalent interactions. These newly designed molecules exhibited noteworthy enhancements in optoelectronic and performance-based metrics than the reference. Almost all molecules showed a bathochromic shift in their absorption profile, with the value of λmax ranging from 612 to 818 nm in chloroform solvent. A remarkable reduction in energy loss value has also been observed in tailored molecules except DN6. New end-capped molecules DN1, DN2, DN3, and DN6 exhibited less bandgap value than the reference. Similarly, DN3–DN5 has remarkable improvements in the value of open circuit voltage and fill factor. In short, almost every newly designed molecule has showcased remarkable outcomes in terms of numerous assessed attributes.
为了增强有机太阳能电池的光伏属性,通过对现有DNO15T分子进行端盖修饰,定制了6种新分子(A-D-A型)。为了评估它们的性质,使用B3LYP/ 6-31G (d,p)泛函的密度泛函理论(DFT)进行了各种计算计算。我们研究了几种几何属性,如态密度(DOS)、偶极矩、激发和结合能、开路电压(VOC)、填充因子、分子静电势、前沿分子轨道排列、跃迁密度矩阵(TDM)、重组能、分子平面度、所有分子(DN1-DN6)与参考DNR的平面度偏差。NCI图和等值面也被用来分析它们的非共价相互作用。与参考分子相比,这些新设计的分子在光电和基于性能的指标上表现出显著的增强。在氯仿溶剂中,几乎所有分子的吸收谱都发生了色移,λmax值在612 ~ 818 nm之间。除DN6外,在定制分子中也观察到能量损失值的显著降低。新的端盖分子DN1、DN2、DN3和DN6的带隙值比参考分子小。同样,DN3-DN5在开路电压值和填充因子上也有显著改善。简而言之,几乎每一个新设计的分子都在许多评估属性方面显示出显著的结果。
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引用次数: 0
Black phosphorus platforms for electrochemical biosensing: stability, functionalization, and wearable applications 电化学生物传感用黑磷平台:稳定性、功能化和可穿戴应用
IF 1.6 4区 化学 Q4 CHEMISTRY, INORGANIC & NUCLEAR Pub Date : 2026-06-03 Epub Date: 2026-02-27 DOI: 10.1080/10426507.2026.2637681
Xingxing Li (Data curation Formal analysis Software Writing – original draft) , Li Fu (Conceptualization Project administration Writing – review & editing) , Fei Chen (Data curation Formal analysis Methodology Writing – original draft) , Yanfei Lv (Formal analysis Validation Visualization) , Shichao Zhao (Investigation Methodology Resources Software) , Hassan Karimi-Maleh (Conceptualization Supervision Visualization Writing – review & editing)
Black phosphorus (BP), a two-dimensional (2D) layered material, has emerged as a highly promising candidate for next-generation electrochemical biosensing platforms. Its unique combination of a layer-tunable direct bandgap, high charge carrier mobility, and pronounced in-plane anisotropy distinguishes it from other 2D materials such as graphene and transition metal dichalcogenides. These intrinsic properties render BP highly responsive to local electronic perturbations, enabling sensitive transduction for low-abundance biological targets. However, practical deployment is severely hampered by rapid degradation under oxygen, water, and light. This review is primarily focused on BP-enabled electrochemical biosensing, emphasizing stability engineering, surface functionalization for biointerfaces, and device integration toward flexible and wearable sensing; imaging or drug-delivery studies are discussed only when they provide transferable stabilization or biocompatibility insights. We analyze BP degradation mechanisms, then compare stabilization strategies with explicit attention to the tradeoffs between physical encapsulation and chemical functionalization (covalent versus non-covalent). We next summarize electrochemical detection across representative analyte classes, spanning small molecules (e.g. neurotransmitters) to macromolecular biomarkers (e.g., nucleic acids and proteins), and we close by outlining wearable integration routes and the remaining barriers for real-world operation in complex biofluids and scalable manufacturing.
黑磷(BP)是一种二维(2D)层状材料,已成为下一代电化学生物传感平台的极有前途的候选者。它独特的结合了层可调的直接带隙,高电荷载流子迁移率,以及明显的平面内各向异性,使其与其他二维材料(如石墨烯和过渡金属二硫族化合物)区别。这些固有特性使BP对局部电子扰动高度敏感,能够对低丰度的生物靶标进行敏感的转导。然而,由于在氧气、水和光线下的快速降解,实际应用受到严重阻碍。这篇综述主要集中在bp驱动的电化学生物传感,强调稳定性工程,生物界面的表面功能化,以及柔性和可穿戴传感的设备集成;成像或给药研究只有在提供可转移的稳定性或生物相容性见解时才会被讨论。我们分析了BP降解机制,然后比较了稳定策略,明确关注物理包封和化学功能化(共价与非共价)之间的权衡。接下来,我们总结了代表性分析物类别的电化学检测,从小分子(如神经递质)到大分子生物标志物(如核酸和蛋白质),最后我们概述了可穿戴集成路线,以及在复杂生物流体和可扩展制造中实际操作的剩余障碍。
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引用次数: 0
Synthesis, spectroscopic characterization, DFT study, and antibacterial evaluation of sulfur-bridged thiazole-, thiadiazole-, and triazine-based heterocyclic scaffolds 硫桥接噻唑、噻二唑和三嗪基杂环支架的合成、光谱表征、DFT研究和抗菌评价
IF 1.6 4区 化学 Q4 CHEMISTRY, INORGANIC & NUCLEAR Pub Date : 2026-06-03 Epub Date: 2026-02-16 DOI: 10.1080/10426507.2026.2632952
Sarathi N. (Data curation Formal analysis Investigation Writing – original draft) , Ashok Kumar S. L. (Methodology) , Saravana Kumar M. (Writing – review & editing) , Satheesh Kumar N. (Data curation) , Rajalakshmi R. (Resources Software)
The development of structurally diverse heterocyclic frameworks remains a cornerstone in the search for new antimicrobial agents. In this work, four sulfur-bridged heterocyclic scaffolds (S1–S4) featuring thiazole, thiadiazole, pyridine, and triazine cores were synthesized using a one-pot base-promoted nucleophilic substitution strategy facilitated by phase-transfer catalysis. Structural elucidation was achieved using spectroscopic techniques, including FT-IR, UV-Visible, 1H,13C NMR, and ESI mass spectrometry. Single-crystal X-ray diffraction data for scaffold S4 confirmed its symmetrical, rigid architecture. The electronic absorption spectra revealed dominant π → π* transitions, consistent with high molecular planarity and delocalized electronic systems. Further insight into the electronic properties of S4 was obtained through density functional theory (DFT) calculations, which supported its extended conjugation and electron-donating potential. Antibacterial studies showed all scaffolds displayed varying inhibition against both Gram-positive and Gram-negative strains, with S4 consistently exhibiting the largest inhibition zones. Although Ciprofloxacin exhibited larger inhibition zones, the consistent measurable activity of S4 highlights it as a promising lead scaffold for future antibacterial development. The favorable performance of S4 is attributed to its highly conjugated structure and physicochemical properties, underscoring the importance of scaffold design in medicinal chemistry. Future molecular docking studies will be undertaken and correlated with in vitro antibacterial results to provide deeper insights into binding interactions and structure–activity relationships.
结构多样的杂环框架的发展仍然是寻找新的抗菌药物的基石。在这项工作中,采用相转移催化促进的一锅碱促进亲核取代策略合成了四个硫桥接杂环支架(S1-S4),其核心为噻唑、噻二唑、吡啶和三嗪。结构解析采用光谱技术,包括FT-IR, uv -可见,1H,13C NMR和ESI质谱。支架S4的单晶x射线衍射数据证实了其对称的刚性结构。电子吸收光谱显示优势π→π*跃迁,符合高分子平面性和离域电子系统。通过密度泛函理论(DFT)计算进一步了解了S4的电子性质,支持了其扩展共轭和给电子势。抗菌研究表明,所有支架对革兰氏阳性和革兰氏阴性菌株均表现出不同的抑制作用,其中S4始终表现出最大的抑制区。虽然环丙沙星表现出更大的抑制区,但S4的一致可测量活性表明它是未来抗菌开发的有前途的先导支架。S4的良好性能归功于其高度共轭的结构和理化性质,这凸显了支架设计在药物化学中的重要性。未来将开展分子对接研究,并与体外抗菌结果进行关联,以更深入地了解结合相互作用和构效关系。
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引用次数: 0
Design, synthesis, bioactivity evaluation, molecular docking, ADMET, and drug-likeness studies of novel thiochroman-4-one derivatives containing a semicarbazone moiety as potential α-glucosidase inhibitors 设计、合成、生物活性评价、分子对接、ADMET和药物相似性研究新型含氨基脲类α-葡萄糖苷酶抑制剂的硫铬-4- 1衍生物
IF 1.6 4区 化学 Q4 CHEMISTRY, INORGANIC & NUCLEAR Pub Date : 2026-06-03 Epub Date: 2026-03-06 DOI: 10.1080/10426507.2026.2641681
Qing Liu (Conceptualization Data curation Methodology Software Writing – original draft) , Jinying Huang (Data curation Methodology Software Writing – original draft) , Wenmin Pan (Data curation Investigation Methodology Software Validation) , Tiantian Zhuang (Conceptualization Data curation Methodology Software Validation) , Xiang Wang (Funding acquisition Project administration Writing – original draft) , Pei Li (Conceptualization Data curation Funding acquisition Methodology Project administration Software Validation Writing – original draft Writing – review & editing)
In this study, a series of novel thiochroman-4-one derivatives incorporating a semicarbazone functional group were successfully synthesized and thoroughly characterized via 1H NMR,13C NMR, and HRMS analyses. Biological evaluations revealed that the synthesized compounds 6a6k exhibited moderate in vitro antioxidant effects, as demonstrated by their ability to scavenge DPPH and ABTS radicals, along with notable α-glucosidase inhibition. Among them, compound 6h stood out with significant in vitro inhibitory potency against α-glucosidase, yielding an IC50 value of 84.65 µg/mL, which was substantially lower than that of acarbose (237.48 µg/mL). The molecular docking analysis revealed that compound 6h interacts strongly with the active site of human intestinal α-glucosidase (PDB ID: 3TOP) via several binding interactions, exhibiting a binding energy of −8.6 kcal/mol. Moreover, the predicted ADMET properties and drug-likeness evaluation suggest that compound 6h possesses promising pharmacokinetic characteristics and a low toxicity risk, fulfilling essential requirements for prospective therapeutic candidates.
在本研究中,成功合成了一系列新的含氨基脲官能团的硫代铬-4- 1衍生物,并通过1H NMR、13C NMR和HRMS分析对其进行了全面表征。生物学评价表明,合成的化合物6a-6k具有中等的体外抗氧化作用,具有清除DPPH和ABTS自由基的能力,并具有明显的α-葡萄糖苷酶抑制作用。其中,化合物6h对α-葡萄糖苷酶的体外抑制能力最强,IC50值为84.65µg/mL,显著低于阿卡波糖(237.48µg/mL)。分子对接分析表明,化合物6h通过多种结合作用与人肠道α-葡萄糖苷酶活性位点(PDB ID: 3TOP)强相互作用,结合能为−8.6 kcal/mol。此外,预测的ADMET性质和药物相似性评估表明,化合物6h具有良好的药代动力学特征和低毒性风险,满足了潜在治疗候选药物的基本要求。
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引用次数: 0
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Phosphorus, Sulfur, and Silicon and the Related Elements
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