Aerobic Benzylic C(sp3)-H Bond Oxygenations Catalyzed by NBS under Visible Light Irradiation.

An efficient photocatalytic oxidation of benzylic C(sp3)-H bonds to ketones, esters, and amides has been developed using NBS as a metal-free photocatalyst and O2 as an oxidant. A variety of synthetically and biologically valuable compounds are assembled in moderate to excellent yields. The synthetic utility of this approach has been demonstrated by gram-scale experiments. A possible free radical mechanism was proposed to rationalize the reaction procedure.

Phytochemistry, nutritional composition, health benefits and future prospects of Passiflora: A review.

Passiflora, also known as "passion fruit", is widely grown in tropical and subtropical regions. It is not only eaten raw but is also widely used in processed foods. Various extracts, juices and isolated compounds show a wide range of health effects and biological activities, such as antioxidant, anti-inflammatory, sedative, and neuroprotective effects. In this review, we not only review the phytochemical properties of Passiflora but also highlight the potential of Passiflora for food applications and the use of all parts as a source of ingredients for medicines and cosmetics that promote health and well-being. This will provide theoretical support for the integrated use of such natural products.

Dioscorea spp.: Bioactive Compounds and Potential for the Treatment of Inflammatory and Metabolic Diseases.

Dioscorea spp. belongs to the Dioscoreaceae family, known as "yams", and contains approximately 600 species with a wide distribution. It is a major food source for millions of people in tropical and subtropical regions. Dioscorea has great medicinal and therapeutic capabilities and is a potential source of bioactive substances for the prevention and treatment of many diseases. In recent years, increasing attention has been paid to the phytochemicals of Dioscorea, such as steroidal saponins, polyphenols, allantoin, and, in particular, polysaccharides and diosgenin. These bioactive compounds possess anti-inflammatory activity and are protective against a variety of inflammatory diseases, such as enteritis, arthritis, dermatitis, acute pancreatitis, and neuroinflammation. In addition, they play an important role in the prevention and treatment of metabolic diseases, including obesity, dyslipidemia, diabetes, and non-alcoholic fatty liver disease. Their mechanisms of action are related to the modulation of a number of key signaling pathways and molecular targets. This review mainly summarizes recent studies on the bioactive compounds of Dioscorea and its treatment of inflammatory and metabolic diseases, and highlights the underlying molecular mechanisms. In conclusion, Dioscorea is a promising source of bioactive components and has the potential to develop novel natural bioactive compounds for the prevention and treatment of inflammatory and metabolic diseases.

Carbocyclization of Heterosubstituted Alkynes via the Memory of Chirality: Access to Cα-Substituted Proline Derivatives.

An efficient strategy for the asymmetric synthesis of Cα-substituted proline derivatives from acyclic α-amino acids has been established. The 5-exo-dig asymmetric cyclization of α-amino ester enolates onto heterosubstituted alkynes provided a product with excellent enantioselectivity via the memory of chirality concept. Density functional theory calculations indicated that a heteroatom is crucial for the success of the asymmetric cyclization because a more stabilized vinyl carbanion is produced. This new method has the potential to enable the rapid asymmetric construction of bioactive molecules containing the pyrrolidine skeleton.

Memory of Chirality in Bromoalkyne Carbocyclization: Applications in Asymmetric Total Synthesis of Hasubanan Alkaloids.

A transition-metal-free 5- exo- dig asymmetric cyclization of α-amino ester enolates onto bromoalkynes provided a product with excellent enantioselectivity via the memory of chirality concept. This strategy was applied to a concise total synthesis of (-)-runanine and a formal synthesis of (-)-8-demethoxyrunanine and (-)-cepharatine D.

Synthesis of Quinolizinium-Type Heteroaromatics via a Carbene Intermediate.

An efficient synthesis of quinolizinium-type heteroaromatics by Pt(II)-catalyzed cyclization of 2-arylpyridine propargyl alcohol has been developed. The presence of a protic acid is crucial for the success of the reaction. Mechanistic studies disclosed that the reaction proceeds via a platinum-carbene intermediate. Additionally, the fluorescence properties of the synthesized heteroaromatics were investigated to provide perspectives for potential applications.

The design, synthesis and in vitro immunosuppressive evaluation of novel isobenzofuran derivatives.

The synthesis and biological evaluation of a series of novel isobenzofuran-based compounds are described. The compounds were evaluated for their immunosuppressive effects of T-cell proliferation and IMPDH type II inhibitor activity in vitro, as well as their structure-activity relationships were assessed. Several compounds demonstrated highly efficacious immunosuppressive properties, especially compounds 2d, 2e, 2h and 2j, which were superior to MPA, while compounds 2k, 2m, 2n, 4c and 5d exhibited an equipotent inhibitory activity compared to MPA. Generally, it was obviously demonstrated that α,ß-unsaturated amides proved more potent than the diamide and urea series. The present study provides a guide for further research on development of safe and effective immunosuppressive agents.