芳香基苯并咪唑衍生物的合成、表征及抑菌活性研究

在微波辐射下,通过二茂铁磺酰氯和相应的苯并咪唑合成了4种芳香基苯并咪唑衍生物。经^1H NMR、MS及元素分析确证产物结构。通过X线衍射测定了化合物4a的晶体结构。用琼脂稀释法测定化合物抑菌活性,并与对照药剂50%多菌灵可湿性粉剂比较,结果表明化合物4a～4d对番茄早疫病菌、烟草赤星病菌和小麦赤霉病菌有与对照药剂近似的抑菌活性。     

壳聚糖水杨酸盐-明胶共混膜结构表征及其抗菌性

以溶液共混法成功制备出壳聚糖水杨酸盐－明胶共浊膜，用FT－IR、XRD、SEM表征了其结构，并测试了其吸水率，力学性能及抑菌性能。结果表明，壳聚糖水杨酸盐－胶胶共混膜中存在强烈的氢键相互作用及良好相容性，共混膜的力学性能随明胶含量增大而明显提高，当明胶含量为30％时，共混膜的抗张强度最大，其干、湿态抗张强度分别达99．9MPa和34．9MPa，比纯壳聚糖膜干，湿态抗张强度分别提高了99．8％有83．75，共浊膜抑菌性随明胶含量增加而下降，但其抑菌性仍明显高于壳聚糖膜。水杨酸的引入有利于改善其力学性能及抗菌性能，该共漫漫经膜作为一种潜在的伤口包扎材料，将具有广阔应用前景。     

Carbazole Derivatives as Potential Antimicrobial Agents

Microbial infection is a leading cause of death worldwide, resulting in around 1.2 million deaths annually. Due to this, medicinal chemists are continuously searching for new or improved alternatives to combat microbial infections. Among many nitrogen-containing heterocycles, carbazole derivatives have shown significant biological activities, of which its antimicrobial and antifungal activities are the most studied. In this review, miscellaneous carbazole derivatives and their antimicrobial activity are discussed (articles published from 1999 to 2022).     

Contribution of Aldehydes and Their Derivatives to Antimicrobial and Immunomodulatory Activities

Essential oils (EOs) are intricate combinations of evaporative compounds produced by aromatic plants and extracted by distillation or expression. EOs are natural secondary metabolites derived from plants and have been found to be useful in food and nutraceutical manufacturing, perfumery and cosmetics; they have also been found to alleviate the phenomenon of antimicrobial resistance (AMR) in addition to functioning as antibacterial and antifungal agents, balancing menstrual cycles and being efficacious as an immune system booster. Several main aldehyde constituents can be found in different types of EOs, and thus, aldehydes and their derivatives will be the main focus of this study with regard to their antimicrobial, antioxidative, anti-inflammatory and immunomodulatory effects. This brief study also explores the activity of aldehydes and their derivatives against pathogenic bacteria for future use in the clinical setting.     

Synthesis and Antimicrobial Evaluation of Some New 1,5-Benzothiazepine Derivatives and Their Ribofuranosides

( - )- cis -2(4-Methoxyphenyl)-3-hydroxy/methoxy-6,8-dichloro/6-chloro-2,3-dihydro-1,5-benzothiazepin-4[5H/5-chloroacetyl/5-(4'-methylpiperazino-1')acetyl]-ones have been synthesized by the condensation of 2-amino-3,5-dichloro/3-chloro benzenethiol with methyl-( - )- trans -3(4-methoxyphenyl)glycidate in xylene. Ribofuranosides viz ( - )- cis -2(4-methoxyphenyl)-3-methoxy-6,8-dichloro/6-chloro-2,3-dihydro-1,5-benzothiazepine-4-[5-(2',3',5'-tri- O -benzoyl- g -D-ribofuranosyl)-ones have been synthesized by the treatment of 3-methoxy derivatives of 1,5-benzothiazepines with sugar viz g -D-ribofuranose-1-acetate-2,3,5-tribenzoate in toluene at vacuo. Synthesized compounds have been characterized by elemental analysis, IR, 1 H NMR spectral studies and screened for their antimicrobial activity.     

New Approaches for the Synthesis of Thiazoles and Their Fused Derivatives with Antimicrobial Activities

The 2‐ethoxy carbonyl methylene thiazol‐4‐one ( 3 ) reacts with acetophenone ( 4 ) to give the ethyl 2‐(4‐oxo‐4,5‐dihydro‐thiazol‐2‐yl)‐3‐phenyl‐2‐butenoate ( 5 ). The reactivity of the latter product towards aromatic aldehydes 6a‐d , cyanomethylene reagents 9a,b , aromatic aldehydes 13a‐d , phenylisothiocyanate ( 16 ), elemental sulfur and aromatic amines ( 20a‐c ) was studied to give arylidene, pyridine, thiophene and anilide derivatives. Some of the newly synthesized derivatives were used to synthesize fused derivatives. The antimicrobial activities of the newly synthesized products were tested in vitro for antimicrobial activity against two bacterial isolates, one saprophytic (Escherichia coli) and the other parasitic (Xanthomonas citri) and for antifungal activity against one saprophytic (Aspergillus fumigatus) and two phytopathogenics (Rhizoctonia solani and Fusarium oxysporum).     

Polysaccharides and Their Derivatives for Versatile Tissue Engineering Application

Research and development in the design, synthesis, modification, evaluation, and characterization of polysaccharide‐based bioactive polymeric materials for guiding and promoting new tissue in‐growth is reviewed. Emphasis is given in this interdisciplinary field of tissue engineering (TE) with particular reference to bone, cartilage, and skin TE. Current strategies in scaffold‐guided TE approaches using polymers of natural origin and their composites are elaborated. Innovative modification techniques in creating functional materials for advanced TE applications are presented. Challenges and possible solutions in the technological innovation in factor molecules incorporation and surface functionalization for improving the fabrication of biomaterials scaffolds for cost‐effective TE are also presented.

     

Synthesis of Some Novel Pyrimidinedione and Pyrimidinetrione Derivatives by a Greener Method: Study of Their Antimicrobial Activity and Photophysical Properties

A series of novel pyrimidinedione- and pyrimidinetriones-based compounds were synthesized by different techniques such as with conventional Knoevenagel condensation alone, with a Rhizopus oryzae lipase biocatalyst, and with a deep eutectic solvent (DES). The yield was found to be maximum by using lipase and DES. Reuse of the lipase and DES was possible up to four consecutive cycles. These methods are mild, highly efficient, and amenable to scaleup. The products were found to exhibit appreciable in vitro antibacterial activity against Echerichia coli, Pseudomonas neumoniae, and Micrococcus and in vitro antifungal activity against Aspergillus niger and Candida albicans. All the compounds exhibited appreciable in vitro activity against the tested strains. The photophysical properties and thermal stability of the products were also investigated.     

Synthesis and Characterization of Chloralose-Derived Thiosemicarbazones and Semicarbazones and Investigation of Their Antimicrobial Properties

Thiosemicarbazones(7–10)/semicarbazones(11–14) were synthesized in good yields via the condensation of α-gluco-, β-gluco-, galacto-, manno- chloralose derived 1,4-furanodialdoses (1-4) with thiosemicarbazide(5)/semicarbazide(6). The structures of all products were characterized by FTIR, NMR spectroscopic methods and elemental analysis. The compounds have been found to display moderate antimicrobial activity against Gram-positive, Gram-negative bacteria and antifungal activity against a Candida albicans. MIC values of the compounds range from 260 to 1510 μg/mL.     

Synthesis and Antimicrobial Studies of Some Quinolinylpyrimidine Derivatives

The quinolinylpyrimidine derivatives were prepared by the condensation of quinolinyl chalcones with urea (or thiourea) under basic conditions by using both conventional and microwave heating. Their IR, ¹H NMR, ¹³C NMR, mass spectra and CHN analyses confirmed the prepared compounds. The newly prepared quinolinylpyrimidine derivatives were screened for antimicrobial activities against the bacterial strains viz. S. aureus, Shigella, Salmonela, P. aeroginosa, B. Subtilus and E. coli and found considerably active against S. aureus, P. aeroginosa and E. coli.     

L-苯丙氨酸衍生物的一锅法合成及其抗/促凝活性

氨基酸及其衍生物在止血/抗凝活性方面有一定的应用。以L-苯丙氨酸为起始原料,经磺化引入磺酸基,再与甲醇、乙醇、丙醇、异丙醇和正丁醇脱水酯化,一锅法合成了6种未见报道的L-苯丙氨酸的磺酸酯类衍生物(L1~L6),以期获得具有的较强血液生理活性的潜在药物。实验中采用了质谱、核磁共振进行结构表征。该合成方法产率高(78%~95%),后处理简单,不失为合成该类衍生物的好方法。衍生物的凝血四项实验表明:抗促凝效果是内源性和外源性凝血途径共同作用的结果。血浆复钙实验表明:衍生物均具有一定的抗凝活性,其抗凝效果随浓度变化而变化,但是随R链的长度增加,抗凝效果并未见规律性。衍生物的抗凝活性主要受磺酸基及酯基的影响,因此在设计合成抗血栓化合物时可以考虑引入磺酸基及酯类基团。     

Biginelli Reaction Mediated Synthesis of Antimicrobial Pyrimidine Derivatives and Their Therapeutic Properties

Antimicrobial resistance was one of the top priorities for global public health before the start of the 2019 coronavirus pandemic (COVID-19). Moreover, in this changing medical landscape due to COVID-19, finding new organic structures with antimicrobial and antiviral properties is a priority in current research. The Biginelli synthesis that mediates the production of pyrimidine compounds has been intensively studied in recent decades, especially due to the therapeutic properties of the resulting compounds, such as calcium channel blockers, anticancer, antiviral, antimicrobial, anti-inflammatory or antioxidant compounds. In this review we aim to review the Biginelli syntheses reported recently in the literature that mediates the synthesis of antimicrobial compounds, the spectrum of their medicinal properties, and the structure–activity relationship in the studied compounds.     

Synthesis and Antimicrobial Activity of Some Annelated Quinazoline Derivatives

A highly efficient and versatile synthetic approach to the synthesis of annelated quinazoline derivatives viz 1,2,4‐triazino[4,3‐c]quinazoline 5–7 , 11 , thiazolidinylquinazoline 9 , quinazolino[4,3‐b]quin‐azolin‐8‐one 12 and imidazoquinazolines 14a,b,15 is presented. Also, a variety of pyrazolylquinazolines 19–21 and pyrimidinylquinazolines 22a,b were obtained via a sequence of heterocyclization reactions of 4‐methyl‐N‐[4‐(4‐oxo‐3,4‐dihydroquinazolin‐2‐yl)phenyl]benzene‐sulfonamide ( 2 ) with different reagents. The new compounds were synthesized with the objective of studying their antimicrobial activity.     

壳聚糖及其衍生物抗菌活性的研究进展

壳聚糖是自然界目前发现的唯一碱性多糖,具有自然来源丰富,生物相容性好,可被生物降解,安全无毒和抗菌性强等许多天然的优良特性,现其广谱抗菌性已得到广泛的认可,但较差的水溶性限制了它的进一步应用。因此,通过一定的改性方法制备壳聚糖衍生物以提高其水溶性,是目前壳聚糖研究方面的热点之一。本论文就近年来几种常见的壳聚糖亲水改性方法及其衍生物在抗菌方面的应用进展进行综述,以期对壳聚糖的深入研究提供参考。     

A Study of the Electrochemistry of Two Biacridine Derivatives and Their Application

The electrochemlcal behavior of two new synthesized biacridine derivatives,3,3’－disulfonyl－9,9’－biacridine dinitrate（DSBADN）and 10,10’－dimethyl－3,3’－disulfonyl－9,9’－biacridine（DMDSBA）was investigated by means of cyclic voltammetry and linear sweep polarography．Ina HCl solution,the reduction peak current was proportional to the concentrations of DSBADNand DMDSBA．The electrochemical study demonstrated that the reduction peak currents ofDSBADN and DMDSBA exhibited adsorptive and diffusion－controlled characteristics,and the     

水溶性量子点的制备及其与壳聚糖衍生物的自组装

以3-巯基丙酸(HS-CH2CH2COOH)为稳定剂, 制备了水溶性的碲化镉(CdTe)量子点(QDs), 考察了制备条件对QDs荧光性能的影响及CdTe QDs与壳聚糖及叶酸和聚乙二醇改性的壳聚糖的自组装. 研究发现, 壳聚糖及改性壳聚糖与QDs的复合物荧光强度相对纯的CdTe QDs明显增强, 且QDs被包裹在内核, 复合粒子呈明显的核/壳结构. 改性壳聚糖/QDs复合物较小且尺寸分布更为均一.     

双金属MOFs及其衍生物在电化学储能领域中的应用

双金属有机骨架及其衍生物一方面具有单金属有机骨架孔道丰富、比表面积大、结构可调、活性位点丰富等特点,另一方面具有双组分与多孔结构之间的协同效应,因而受到了研究人员的密切关注,在储能、催化、分离、传感器、医药、气体存储等领域广泛应用。和单金属MOFs类似,双金属MOFs的导电性不佳、结构易坍塌,这极大地限制了其在电化学储能中的应用。通过对双金属MOFs进行热处理,易得到分布均匀的多孔碳@双金属氧化物/硫化物/磷化物/硒化物等衍生物,不仅保持了独特的多孔结构,而且提高了材料的导电性和结构稳定性,有利于在电化学储能中的应用。因此,本文从双金属MOFs中的主要金属离子入手,综述了双金属MOFs及其衍生物用于超级电容器、锂离子电池、钠离子电池、金属空气电池等电化学储能器件的最新应用进展。在此基础上,总结了双金属MOFs在电化学储能应用中的优势,并对其制备、作用机理和后处理研究提出了建议。     

A Facile Synthesis of Bromo-Substituted Benzofuran Containing Thiazolidinone Nucleus Bridged with Quinoline Derivatives: Potent Analgesic and Antimicrobial Agents

Treatment of 5-bromo-2-acetyl benzofuran with hydrazine followed by condensation of the resulting hydrazone with different quinoline derivatives gave the corresponding Schiff bases. Reaction of these Schiff bases with thioacetic acid furnished the target thiazolidinone molecule. Some of the newly synthesized compounds show promising analgesic and antimicrobial activity.

Supplemental materials are available for this article. Go to the publisher's online edition of Phosphorus, Sulfur, and Silicon and the Related Elements to view the free supplemental file.     

EDTA二酐及其衍生物

本文综述了EDTA二酐及其衍生物的合成、性质和应用。