Amphiphilic tri-arm star-shaped copolymers, poly(ethylene oxide)-b-poly(ε-caprolactone) PEO3-b-PCL3, with different poly (ε-caprolactone) (PCL) molecular weights were successfully synthesized by ring-opening polymerization (ROP). Firstly, the tri-arm star-shaped PEO3 was prepared by ROP of trimethylolpropane and ethylene oxide (EO). The ring-opening polymerization (ROP) of ε- caprolactone (CL) was initiated using the tri-arm star-shaped PEO3 with the hydroxyl group as macroinitiator and Sn(Oct)2 as a catalyst. Amphiphilic tri-arm star-shaped copolymers PEO3-b-PCL3 were obtained. By changing the ratio of monomer and macroinitiator, a series of PEO3-b-PCL3 were prepared with a well-defined structure, molecular weight control, and narrow molecular weight distribution. The expected intermediates and final products were confirmed by 1H NMR and Gel Permeation Chromatography (GPC) analyses. In addition, the sizes and morphologies of the obtained micelles with different PCL segment lengths were investigated with dynamic light scattering (DLS) and transmission electron microscopy (TEM), respectively. It was found that the self-assembly morphologies were spherical micelle in aqueous solution.

A novel series of coumarin-benzimidazole hybrids were designed, synthesized, and extensively characterized using spectral data, including FT-IR, 1H-NMR, and 13C-NMR. Weatherburn's method was used to test new compounds' inhibition of urease activity. The results were evaluated by considering the effects of different side groups and hybridization. The chlorine atom in the molecules notably affects the inhibitory activity of urease. The best result was obtained with the compound “6- chloro-N'-{[5,6-dichloro-2-(2-thienylmethyl)-1H-benzimidazol-1-yl]acetyl}-2-oxo-2H-chromene-3- carbohydrazide” (3b) with IC50= 12.48±0.12 μg/mL against Jack bean urease.

Introduction: A newly designed heterogeneous copper catalytic platform immobilizing copper (II) salt on chitosan Schiff base-modified carbon nanotubes was developed (Cu@CS-Py@CNT). Method: The structure of the catalyst platform was fully characterized by spectroscopic analyses. Result: The catalytic activity of the Cu@CS-Py@CNT was investigated in a one-pot synthesis of 1,4-disubstituted 1,2,3-triazoles by the regioselective click reaction using various benzyl halides or their surrogates, terminal alkynes, and sodium azide in an aqueous environment without using any external Cu-reducing agents.

Background: Irritant, expensive, or toxic desulfurating agents are usually used in the synthesis of isothiocyanates from amines, CS2, and appropriate bases, accompanied by a tedious workup. A more practical and green method has been developed. Methods: Cheap and non-toxic CaO was used as both a base and a desulfurating agent in the synthesis of isothiocyanates. Results: Both alkyl and aryl isothiocyanates are easily synthesized in moderate to high yield from amines, CS2, and CaO under mild conditions. Conclusion: A simple and practical synthetic approach for isothiocyanates from amines, CS2, and CaO was developed. CaO acts as both a base and a desulfurating agent in the reactions, simplifying the reaction system and reducing cost as well as side products. Moderate to high yields were obtained at room temperature in 48 hours which included alkyl and aryl isothiocyanates.

: Natural products have been created by nature and are derived from organisms such as plants or microorganisms. The natural compounds are isolated from natural sources in very small quantities, making it difficult for the form to achieve the compounds' good yields. The last is relevant for doing biological essays and chemical structure elucidation. Besides, they have diverse chemical structures, which have inspired organic chemists to do their organic synthesis. It is important to construct a strategy based on a well-designed retrosynthesis. The reproducibility of the selected methodology, the yields of the compounds of each step and stereoselectivity or diastereoselectivity of the reactions that are being used are the main key points to guarantee the success of a natural compound synthesis. Modern technologies can be the solution. In this review, we try to compile in the form of a critic perspective the most modern techniques that organic chemists are applying for the synthesis of complex natural compounds.

Artificial enzyme mimics have lately sparked a lot of attention since they offer a lot of benefits over natural enzymes. Because of their proteic origin and tailorable structures, self-assembling peptides are ideal building blocks for the creation of artificial enzymes. Recently, a series of histidinebearing self-assembling peptides with β-sheet structures, which are selective for short-chain fatty acids, were described. In this work, the catalytic behaviors of these peptides were further investigated using 2,4-dinitrophenyl acetate (DNPA) as a model substrate. Furthermore, the peptide was capable of forming a solid hydrogel that was also catalytically active at higher concentrations.

Specific recognition at trace quantity levels of metal ions without using the costly analytical instrument and a tedious sample preparation method is an extensive concern for environmental monitoring and mitigation. Mercury(II) (Hg2+) has acute toxicity. The development of ion-selective fluorescence sensors for the selective detection of Hg2+ is an essential task to accomplish. The aim of this study is to detect Hg2+ in an aqueous medium. A fluorescence sensor (DP) based on Schiff base was designed and utilized to detect Hg2+. Scanning electron microscope (SEM), Fourier transformed Infrared (FT-IR), X-ray powder diffraction (XRD), and X-ray photoelectron spectroscopy (XPS) were used to learn the sensing mechanism between sensor DP and Hg2+ cations. When Hg2+ ions were added to the sensor DP, it showed a dramatic fluorescent “turn-on” response for Hg2+ in dimethylformamide (DMF) solution. And the detection limit (LOD) of DP for Hg2+ in aqueous media (1.0 mol L-1) was 2.23 × 10-8 mol L-1. In summary, an aminoantipyrine-containing Schiff base fluorescent chemosensor for extraordinary recognition of Mercury(II) was designed and synthesized via a simple one-step pathway and led to intermolecular self-assembly through π-π stacking interactions. And the sensor DP could fluorescently “turn on” when the Hg2+ cation was added. The limitation of Hg2+ was 2.23×10-8 M, which indicated that the sensor DP could be useful as a highly selective and sensitive sensor for detecting Hg2+ ions in an aqueous medium by the strong interaction with DP. Notably, the sensor DP was used as a fluorescent display material with satisfactory results.

Introduction: The Morita-Baylis-Hillman (MBH) reaction is an important method for forming carbon-carbon bonds between carbonyl-containing compounds and activated olefins. However, the slow reaction rate with electron-rich electrophilic partners has limited its wider use. To overcome this drawback, the effects of pyridinium-based ionic liquids mediated quinuclidine catalytic system for MBH reactions were studied. Method: The method is simple, involving neat and open-flask conditions, and is compatible with a wide range of reagents. We offered general pyridinium-based ionic liquids-mediated quinuclidine catalysis mechanism that is responsible for the observed rate increase. The synthetic versatility of the MBH adducts is demonstrated by the synthesis of important building blocks for the natural product (-)-sitophilure. The authors anticipate that this pyridinium-based ionic liquids-mediated quinuclidine protocol could serve as a general methodology for the MBH reaction. Result: In summary, the study presents a simple and effective method to enhance the reaction rate of the MBH reaction. The authors believe this method has the potential for broader applications and may contribute to developing new synthetic strategies for organic synthesis. Conclusion: We successfully recycled the catalytic system up to 7 runs without losing any catalytic activity.

The first synthesis of 2-bromogentisyl alcohol, a halogenated compound cytotoxicity to breast cancer cell line, was achieved in four steps. Key steps include (i) formylation of aromatic compound, (ii) bromination, (iii) demethylation and (iv) reduction. Compound 3 was prepared from 4- methoxyphenol (2) in 92% yield in the presence of MgCl2 and Et3N, then intermediate 4 was obtained by bromination of 3 in 78% yield. Subsequently, the direct demethylation of 4 with BBr3 afforded the intermediate 5 in 72% yield. Finally, title compound 1 was prepared by the reduction of 5 using NaBH4 in 87% yield. The overall yield is 45% from 4-methoxyphenol. This method is simple and the reaction conditions are mild.

Indole is an important heterocyclic molecule having a number of pharmacologically useful properties. Adolf von Baeyer synthesized indole by reducing oxindole in the presence of a catalytic amount of zinc dust in 1866. A number of studies have been conducted and many more are in the pipeline to investigate the medicinal potential of indole and its derivatives. Indomethacin, Indolmycin, Oxypertine, Yohimbine, Pindolol, and Delavirdine are indole containing drugs that are in high demand in the market. The present study aims to highlight the indole nucleus containing drugs developed by researchers over the last 25 years, with a focus on antibacterial and antifungal properties present in these drugs. The mode of action and Structure–Activity Relationship (SAR) of indole derivatives, which are responsible for antibacterial and other relevant actions, are also highlighted in the present review. To aid scientists in exploring future potential in this domain, the present study includes the key qualities and highlights of each research activity done by researchers especially related to synthetic derivatives of Indoles. All the available information on Indole derivatives was collected via electronic search (using Pubmed, SciFinder, Scirus, Google Scholar, and Web of Science) and the resources available in Central Library, IFTM University, Moradabad were also referred. The present review is based on literature collected and studied over the previous 23 years. This article will aid researchers in the development of new molecules with indole derivatives undoubtedly which must have improved antibacterial and other properties.

: Chalcones are important scaffolds in the field of medicinal chemistry due to the presence of α,β-unsaturated ketone functionality. They are usually synthesized by reacting an aldehyde with acetophenone in the presence of acid or base using the Claisen-Schmidt condensation reaction. Numerous chalcone derivatives have been developed due to the simplicity of their synthesis, and they have intriguing biological activity that has clinical implications for a range of disorders. The review article discusses the advancements made since 2005 for the synthesis of chalcones derivatives using environmentally friendly methods such as the use of green catalysts and solvents, ultrasonic radiation, microwave energy, and methodologies involving grinding in the absence of solvents.

INTRODUCTION: The stereochemical characteristics of spirofused and their derivatives have recently attracted a great deal of interest in synthetic organic chemistry METHOD: A series of ecologically acceptable spirofused heterocycle compounds S(K1–K8) were made using a one- pot microwave irradiation and were characterized by FTIR, 1HNMR, and Mass Spectroscopy. The Iodine-catalyzed Biginelli-type condensation process has been used to synthesize novel anti-microbial and anthelmintic potential spiroketals (spirofused) derivatives by using a fast, safe & effective microwave irradiation approach in order to get the product in maximum yield with lesser time consumption. RESULT: The compounds SK4 and SK5 showed promising antimicrobial activity against all bacterial (Bacillus subtilis, Staphylococcus aureus, Pseudomonas aeruginosa, Escherichia coli) and fungal strains (Candida albicans and Aspergillus niger) with MIC 6.25 µg/mL and 12.5 µg/mL. Furthermore, molecular docking studies were also simulated for compounds SK4 and SK5 to predict the specific binding mode of these compounds. CONCLUSION: Albendazole (Alb) was used as a reference medicine to test the anthelmintic activity of Indian adult earthworms Eisenia fetida. Compound SK4 has been found to be an effective pharmacophore.

Introduction: In this work, we have successfully synthesized four types of ionic liquid-mediated Pd nanocatalysts and performed the physiochemical analysis of the developed Pd-based nanocatalysts using a transmission electron microscope (TEM), X-Ray diffraction analysis (XRD), X-ray photoelectron spectroscopy (XPS), and atomic absorption spectroscopy (AAS) analysis. Method: The well-dispersed and fine Pd nanoparticles were recorded in the ILPdNPs-4 catalytic system. We used this catalytic system to reduce a series of aliphatic and aromatic compounds with nitro groups and developed various biologically active amine molecules. In the continuation of the same, we also reduced nitrolactone, which is considered one of the important starting materials for the synthesis of renin inhibitor aliskiren (Tekturna®, and worldwide as Rasilez®). Result: We also completed the catalyst stability test and recycled the ILPdNPs-4 catalytic system for up to eight runs. Conclusion: No sign of metal leaching, Pd black formation, and agglomeration was recorded during recycling runs.

A simple and efficient synthesis of pyrrolo[1,2-a]pyrazine using Schiff base formation, intramolecular cyclization (or N-alkylation), and Pictet–Spengler type reaction (hetero-aromatisation) has been developed. In this chemistry, metal-free, cost and time-effective processes have been highlighted to afford the complex nitrogenous scaffold using simple starting materials.

A new 4-amino-5-mercapto-3-[(1H-indol-3-yl)propyl]-1,2,4-triazole was synthesized from the fusion of indole-3-butyric acid with thiocarbohydrazide. The reaction of 1,2,4-triazole with a series of benzaldehydes afforded the corresponding Schiff bases (2a-2s). All the synthesized compounds were evaluated for their antibacterial activities using a 96-well microbroth dilution assay. The results of the antibacterial activity revealed that Schiff base 2p with both chloro groups at meta and para positions of the phenyl exhibited significant inhibition against Bacillus cereus and Staphylococcus aureus at MIC 9.11 μmol/mL and against Bacillus subtilis spizizenni at 18.20 μmol/mL.

Background: The newly synthesized fluorinated chalcone derivatives are observed to possess antioxidant potential. Method: Two new fluorinated chalcone compounds were effectively synthesized using the Claisen-Schmidt condensation reaction and were recrystallized using the slow evaporation method. The single crystal structure of the compounds was determined and refined through the X-ray single crystal diffraction method. All compounds were subjected to computational structural characterization and Hirshfeld surface analysis. The compounds were then further characterized through the Ultraviolet-visible (UV-Vis) spectroscopic study. The chalcone derivatives were further analysed with biological experimentation and simulation such as in vitro antioxidant (DPPH) assay, molecular docking and in silico ADMET study. Result: The crystal packing revealed that the molecules in the compounds were linked together through the intermolecular C—H•••O and C—H•••π interactions. Hirshfeld surface analysis validated the presence of intermolecular interactions in crystal packing. The UV-Vis spectroscopic study revealed that the absorption wavelength of the compounds that range from 421.79 to 428.98 nm was within the visible region with the energy gap value of 2.58 to 2.62 eV. The DPPH assay disclosed weak antioxidant activity of both compounds (-31 to 20 %, 10000 µg/mL) compared to the standard ascorbic acid (94.5 %, 50 µg/mL). The binding energy of the docked complex inside the target protein, 2CAG was within the range of -7.3 to -7.5 kcal/mol. In the silico model, SwissADME predicted that the two compounds have overall good drug-like properties. Conclusion: Different substituents, more planar configuration and high intramolecular interactions in the crystal packing played their role in increasing the antioxidant activities, binding energy and drug likeliness of the synthesized compounds.

It is common knowledge that cancer is the world's biggest cause of mortality. This has led to the ongoing introduction and validation of new cancer therapy outcomes. Benzimidazole derivatives control DNA stability and cell cycle advancement. A heterocyclic nucleus is structurally more favourable for a direct DNA connection and, thus, for the management of the DNA replication process. This review seeks to explore the usefulness of such drugs in the future facets of cancer prognosis and treatment in addition to discussing the role of benzimidazole in cancer therapy. Benzimidazole derivatives have been reported as a pertinent therapeutic strategy to modify cancer progression and malignancy in the data from 2013 to 2022. Here, we emphasize these features in several cancer types and cell lines using in vitro and in vivo methods.

A three-component reaction under ultrasound irradiation and with a catalytic amount of citric acid was presented for the synthesis of a series of 2-aryl-quinazolin-4(1H)-ones with excellent efficiency and short reaction time. This one-pot reaction with 2-aminobenzonitrile, ammonium hydroxide or glycine and benzaldehydes is a clean and safe route for the environment at room temperature. Mild reaction conditions, green environment, excellent performance, simple method and reduction of environmental consequences are the advantages of the present method. The structures of many synthesized 2-aryl-quinazolin-4(1H)-one compounds were confirmed by 1H, 13C NMR and FTIR spectral data and elemental analysis.

A new phenol derivative, 3-butyryl-2,6-dihydroxy-4-methoxyphenethyl acetate (1) and seven known phenol analogs (2-8) have been isolated from Arctic fungus Phoma muscivora CPCC 401424. Their structures were elucidated by means of extensive spectroscopic analyses (HRMS, NMR, and IR), and comparison with reported data. All compounds were obtained from Phoma muscivora CPCC 401424 for the first time. Compounds 1 and 5 displayed excellent anti-influenza A virus activities with IC50 values of 2.20 and 2.17 μM, respectively. Compounds 1, 2, 5, and 7 showed moderate cytotoxic activities against Hela and H460 cancer cell lines.

Firstly, 2-amino aromatic ketones were synthesized by o-acylation ofp-substituted anilines with nitrile under Sugasawa conditions, and the yield was up to 90.1%. Then, 4-pyridinylquinoline derivatives were synthesized by Friedlander reaction with α-methylene ketones, and the yield was up to 81.9%. The structures of five 2-amino aromatic ketones and eighteen substituted quinolines were characterized by MS, 1H NMR, and 13C NMR. The structures were further confirmed by single crystal X-ray diffraction, which was consistent with the expected structures. Analyzing the crystal structure, it was found that compounds 4j and 4q crystallized in the monoclinic with the P21/n space group, respectively. Compounds 2c, 2d, 2e, and 4n crystallized in the triclinic with the P-1 space group, respectively. Of which compound 4n crystallized in the triclinic space group P-1 with two crystallographically independent but chemically equivalent molecules in the asymmetric unit. The two independent molecules were found to possess different orientations of the chlorine, methyl, pyridyl, and acetyl groups relative to the core (quinoline) two-ring system. This work provides a simple, straightforward synthetic protocol for preparing 4-pyridinylquinoline derivatives.