5-(3\'-Indolyl)oxazole moiety is a privileged heterocyclic scaffold, embedded in many biologically interesting natural products and potential therapeutic agents. Compounds containing this scaffold, whether from natural sources or synthesized, have demonstrated a wide array of biological activities. This has piqued the interest of synthetic chemists, leading to a large number of reported synthetic approaches to 5-(3\'-indolyl)oxazole scaffold in recent years. In this review, we comprehensively overviewed the different biological activities and chemical synthetic methods for the 5-(3\'-indolyl)oxazole scaffold reported in the literatures from 1963 to 2024. The focus of this study is to highlight the significance of 5-(3\'-indolyl)oxazole derivatives as the lead compounds for the lead discovery of anticancer, pesticidal, antimicrobial, antiviral, antioxidant and anti-inflammatory agents, to summarize the synthetic methods for the 5-(3\'-indolyl)oxazole scaffold. In addition, the reported mechanism of action of 5-(3\'-indolyl)oxazoles and advanced molecules studied in animal models are also reviewed. Furthermore, this review offers perspectives on how 5-(3\'-indolyl)oxazole scaffold as a privileged structure might be exploited in the future.

OBJECTIVE: In this study, we have synthesized 19 Thiazolidine (TZD) derivatives to investigate their potential anti-ZIKV effects.
METHODS: Nineteen thiazolidine derivatives were synthesized and evaluated for their cytotoxicity and antiviral activity against the ZIKA virus.
RESULTS: Among them, six demonstrated remarkable selectivity against the ZIKV virus, exhibiting IC50 values of <5μM, and the other compounds did not demonstrate selectivity for the virus. Interestingly, several derivatives effectively suppressed the replication of ZIKV RNA copies, with derivatives significantly reducing ZIKV mRNA levels at 24 hours post-infection (hpi). Notably, two derivatives (ZKC-4 and -9) stood out by demonstrating a protective effect against ZIKV cell entry. Informed by computational analysis of binding affinity and intermolecular interactions within the NS5 domain\'s N-7 and O\'2 positions, ZKC-4 and FT-39 displayed the highest predicted affinities. Intriguingly, ZKC-4 and ZKC-9 derivatives exhibited the most favorable predicted binding affinities for the ZIKV-E binding site.
CONCLUSIONS: The significance of TZDs as potent antiviral agents is underscored by these findings, suggesting that exploring TZD derivatives holds promise for advancing antiviral therapeutic strategies.

This review portrays a comparison between green protocols and conventional nanoparticle (NP) synthesis strategies, highlighting each method\'s advantages and limitations. Various top-down and bottom-up methods in NP synthesis are described in detail. The green chemistry principles are emphasized for designing safe processes for nanomaterial synthesis. Among the green biogenic sources plant extracts, vitamins, enzymes, polysaccharides, fungi (Molds and mushrooms), bacteria, yeast, algae, and lichens are discussed. Limitations in the reproducibility of green protocols in terms of availability of raw material, variation in synthetic protocol, and selection of material due to geographical differences are elaborated. Finally, a conclusion is drawn utilizing green chemical principles, & a circular economy strategy to minimize waste generation, offering a promising framework for the synthesis of NPs emphasizing sustainability.

The increasing resistance of agricultural pests to existing acaricides presents a significant challenge to sustainable agriculture. Therefore, this study introduced FM-1088, a novel isoindolinone-based phenyl trifluoroethyl thioether derivative generated through an innovative design strategy combining bioisosterism and novel cyclization methods. We synthesized several compounds and evaluated their acaricidal efficacy against Tetranychus cinnabarinus in greenhouses and Panonychus citri in field settings. FM-1088 emerged as a standout candidate, demonstrating a lower median lethal concentration (LC50) of 0.722 mg/L compared to the commercial acaricide, cyetpyrafen. Notably, 30 days after application, FM-1088 showed a field control efficacy of 96.4% against P. citri, highlighting its potential for broader applications. The results underscore the utility of the isoindolinone scaffold in pesticide development, offering a promising solution to combat pest resistance with implications for enhanced crop protection and agricultural productivity. Future studies should explore the detailed mode of action of FM-1088 and its potential applicability across diverse agricultural settings, further confirming its role as a sustainable solution for pest management.

Nanoplastics (NPs) generated from plastic debris weathering pose a significant threat to ecosystems. The ubiquity of plastics driven by their advantageous physical properties, necessitates the development of efficient degradation and removal methods. Polystyrene (PS), a common and hazardous aquatic NP is a long-chain hydrocarbon with alternating phenyl groups. This study investigates the photooxidative degradation of PS NPs under UV light irradiation using synthesized MoO3 nanoflakes, nanobelts, and MoO3/SWCNT nanocomposites. Raman spectroscopy, X-ray diffraction, atomic force microscopy, high-resolution transmission electron microscopy, energy dispersive X-ray, Brunauer-Emmett-Teller, and UV-vis spectroscopy were employed to characterize the photocatalyst. Field emission scanning electron microscopy was used to visualize morphological changes in the spherical PS NPs upon interaction with the photocatalysts. MoO3 nanoflakes acting as a photocatalyst under UV irradiation for 24 h achieved an impressive degradation efficiency exceeding 19%. This treatment significantly reduced the average diameter of PS NPs from 220 to 178 nm. Notably, even higher degradation efficiencies were observed with MoO3 nanobelts and nanocomposites as a complete change in the spherical morphology of PS NPs is observed. Fourier transform infrared spectroscopy elucidated the chemical transformations of PS during degradation. The observed changes in PS NPs structure due to photocatalytic oxidation at different time intervals indicate a promising approach.

Aldehyde dehydrogenases (ALDHs) are a family of enzymes that aid in detoxification and are overexpressed in several different malignancies. There is a correlation between increased expression of ALDH and a poor prognosis, stemness, and resistance to several drugs. Several ALDH inhibitors have been generated due to the crucial role that ALDH plays in cancer stem cells. All of these inhibitors, however, are either ineffective, very toxic, or have yet to be subjected to rigorous testing on their effectiveness. Although various drug-like compounds targeting ALDH have been reported in the literature, none have made it to routine use in the oncology clinic. As a result, new potent, non-toxic, bioavailable, and therapeutically effective ALDH inhibitors are still needed. In this study, we designed and synthesized potent multi-ALDH isoform inhibitors based on the isatin and indazole pharmacophore. Molecular docking studies and enzymatic tests revealed that among all of the synthesized analogs, compound 3 is the most potent inhibitor of ALDH1A1, ALDH3A1, and ALDH1A3, exhibiting 51.32%, 51.87%, and 36.65% inhibition, respectively. The ALDEFLUOR assay further revealed that compound 3 acts as an ALDH broad spectrum inhibitor at 500 nM. Compound 3 was also the most cytotoxic to cancer cells, with an IC50 in the range of 2.1 to 3.8 µM for ovarian, colon, and pancreatic cancer cells, compared to normal and embryonic kidney cells (IC50 7.1 to 8.7 µM). Mechanistically, compound 3 increased ROS activity due to potent multi-ALDH isoform inhibition, which increased apoptosis. Taken together, this study identified a potent multi-isoform ALDH inhibitor that could be further developed as a cancer therapeutic.

Vinyl sulfones, with their exceptional chemical properties, are known as the \"chameleons\" of organic synthesis and are widely used in the preparation of various sulfur-containing structures. However, their most alluring feature lies in their biological activity. The vinyl sulfone skeleton is ubiquitous in natural products and drug molecules and boasts a unique molecular structure and drug activity when compared to conventional drug molecules. As a result, vinyl sulfones have been extensively studied, playing a critical role in organic synthesis and pharmaceutical chemistry. In this review, we present a comprehensive analysis of the recent applications of vinyl sulfone structures in drug design, biology, and chemical synthesis. Furthermore, we explore the prospects of vinyl sulfones in diverse fields, offering insight into their potential future applications.

Lysergic acid diethylamide (LSD) analogs have emerged as new psychoactive substances (NPS) since the mid-2010s, and new compounds continue to emerge for recreational use. Since the end of 2023, \"1D-AL-LAD\" appeared on X (formerly Twitter) and other websites. As for the compound \"1D-LSD\" (which also has \"1D\" in the name), several studies show that the ingredient of seized blotter paper printed \"1D-LSD\" was actually 1-(2-thienoyl)-LSD (1T-LSD). However, there are no reports of seizures of 1-(1,2-dimethylcyclobutanecarbonyl)-LSD (1D-LSD). Accordingly, it was considered that all or at least a certain percentage of \"1D-AL-LAD (1-(1,2-dimethylcyclobutanecarbonyl)-6-allyl-nor-LSD)\" is actually 1-(2-thienoyl)-6-allyl-nor-LSD (1T-AL-LAD). This compound is handled by a number of distributors as of April 2024; therefore, it should be characterized in advance if seized. In this study, 1T-AL-LAD was synthesized and characterized using nuclear magnetic resonance spectroscopy, Fourier transform-infrared spectroscopy, liquid chromatography/high-resolution mass spectrometry (LC/HRMS) and gas chromatography/MS (GC/MS). This compound was easily distinguished from previously reported lysergamides. There were some differences in the detectability of 1T-AL-LAD compared with other lysergamides using GC/MS and the fragmentation patterns in LC/HRMS. These differences can be reasonably explained. This information will be of help to determine this substance in seized materials should it emerge on the market.

2-phenylethanol (2-PE), an aromatic alcohol with a rose fragrance, is the second most widely used flavoring substance in the world. It is widely used in the cosmetic, food, and pharmaceutical industries. This paper introduces the chemical synthesis methods of 2-PE and the synthetic pathways in plants and microorganisms, summarizes the strategies to improve the microbial synthesis of 2-PE, reviews the research progress in de novo synthesis of 2-PE in microorganisms, and makes an outlook on the research prospects, aiming to provide a theoretical basis for the industrial production of 2-PE.

Cytidine-5\'-diphosphate choline (CDP-choline) plays a crucial role in the formation of the phospholipid bilamolecular layer in cell membranes and the stabilization of the neurotransmitter system, acting as a precursor to phosphatidylcholine and acetylcholine. CDP-choline has been found effective in treating functional and consciousness disorders resulting from brain injury, Parkinson\'s disease, depression and glaucoma, and other conditions. As such, CDP-choline is widely utilized in clinical medicine and health care products. The conventional chemical synthesis process of CDP-choline is gradually being replaced by biosynthesis due to the expensive and toxic reagents involved, the production of various by-products, and the high cost of industrial production. Biosynthesis of CDP-choline offers two strategies: microbial fermentation and biocatalysis. Microbial fermentation utilizes inexpensive raw materials but results in a relatively low conversion rate and requires a complex separation and purification process. Biocatalysis, on the other hand, involves two stages: the growth of a living \"catalyst\" and the conversion of the substrate. Although the synthetic process in biocatalysis is more complex, it offers a higher conversion ratio, and the downstream processing technique for extraction is relatively less costly. Consequently, biocatalysis is currently the primary strategy for the industrial production of CDP-choline. This review aims to summarize the progress made in both chemical synthesis and biosynthesis of CDP-choline, with particular focus on the metabolic pathway and the synthetic processes involved in biocatalysis, in order to provide insights for the industrial production of CDP-choline.