Mild and efficient synthesis of benzothiazolopyrimidine derivatives CuAAC/ring cleavage/cyclization reaction.

An operationally mild and efficient synthesis of benzothiazolopyrimidine is achieved by a three-component reaction of 2-aminebenzo[]thiazoles, sulfonyl azides and terminal ynones. This cascade process involved a CuAAC/ring cleavage/cyclization reaction. Particularly, most of the benzothiazolopyrimidine derivatives could be isolated by filtration without further purification.

Good adaptability of freshmen in medical universities under the Coronavirus 2019 pandemic: a questionnaire-based single center study in China.

Objective: To investigate the adaptability of freshmen in medical universities to the Coronavirus Disease 2019 (COVID-19) pandemic and to understand the relevant factors affecting their adaptation in medical university.

Methods: Freshmen in a medical university in Guangdong Province were selected and surveyed using a self-administered general questionnaire and a college student adjustment scale prepared by Fang Xiaoyi et al. The results were analyzed statistically.

Copper-catalyzed three-component reaction to synthesize polysubstituted imidazo[1,2-]pyridines.

An efficient three-component one-pot and operationally simple cascade of 2-aminopyridines with sulfonyl azides and terminal ynones is reported, providing a variety of polysubstituted imidazo[1,2-]pyridine derivatives in moderate to excellent yields. In particular, the reaction goes a through CuAAC/ring-cleavage process and forms a highly active intermediate α-acyl--sulfonyl ketenimine with base free.

2-Methoxy-1,4-naphthoquinone regulated molecular alternation of revealed by high-dimensional biological data.

Fungi and the toxins it produces are hazardous to agricultural plants, animals, and human health. However, there is a lack of more effective and environment-friendly natural anti- agents. In the search for natural anti-fungal agents, we found that naturally originated 2-methoxy-1,4-naphthoquinone (MNQ) with a minimal inhibitory dose of 8.

Rapid and efficient synthesis of formamidines in a catalyst-free and solvent-free system.

An operationally rapid and efficient synthesis of -sulfonyl formamidines that proceeds under mild conditions was achieved by reaction of a mixture of an amine, a sulfonyl azide, and a terminal ynone under catalyst-free and solvent-free conditions. Terminal ynones provide the C source to formamidines complete cleavage of C[triple bond, length as m-dash]C.

A simple and efficient copper-catalyzed three-component reaction to synthesize ()-1,2-dihydro-2-iminoquinolines.

A operationally simple synthesis of ()-1,2-dihydro-2-iminoquinolines that proceeds under mild conditions is achieved by copper-catalyzed reaction of 1-(2-aminophenyl)ethan-1-ones, sulfonyl azides and terminal ynones. In particular, the reaction goes through a base-free CuAAC/ring-opening process to obtain the -configured products due to hydrogen bonding.

Targeting ferroptosis for cancer therapy: iron metabolism and anticancer immunity.

Ferroptosis is a new form of programmed cell death characterized by iron-dependent accumulation of lipid peroxidation, which plays an important role in cancer biology. Ferroptosis is involved in many biological processes, such as amino acid metabolism, glutathione metabolism, iron metabolism, and lipid metabolism. Iron is an essential trace element in a variety of normal cell processes, such as DNA synthesis and repair, cell respiration, metabolism and signal transduction, etc.

Pathologic role of peptidyl-prolyl isomerase Pin1 in pulmonary artery remodeling.

Peptidyl-prolyl isomerase Pin1 is crucial for cell proliferation, but its role in pulmonary artery remodeling (PAR) is unclear. In the present study, we aimed to evaluate the expression and contribution of Pin1 in PAR. Treatment with Pin1 inhibitor Juglone or Pin1-specific siRNAs ameliorated the expression of Pin1 and proliferating cell nuclear antigen (PCNA) in human pulmonary artery smooth muscle cells (PASMCs) , and Juglone treatment arrested the cell cycle at the G1 phase.

Preparation of 1,2-substituted benzimidazoles a copper-catalyzed three component coupling reaction.

1,2-Substituted benzimidazoles were prepared by simply stirring a mixture of copper catalysts, -substituted -phenylenediamines, sulfonyl azides and terminal alkynes. Particularly, the intermediate -sulfonylketenimine occurred with two nucleophilic addition and the sulfonyl group was eliminated cyclization. In a way, sulfonyl azides and copper catalysts activated the terminal alkynes to synthesize benzimidazoles.

Potential therapeutic targets and molecular details of anthocyan-treated inflammatory bowel disease: a systematic bioinformatics analysis of network pharmacology.

Anthocyans, containing anthocyanins and anthocyanidins, play a crucial role in preventing and treating inflammatory bowel disease (IBD). Most anthocyanins and their basic elements, namely anthocyanidins have been recognized for the effective treatment of IBD, but the key biomarkers of anthocyan-treated IBD remain unclear. In this study, a bioinformatics analysis based on network pharmacology was performed to demonstrate the core-targets, biological functions, and signaling pathways of most common anthocyanidins that existed in anthocyans to reveal their potential or major mechanisms.

Structural features, interaction with the gut microbiota and anti-tumor activity of oligosaccharides.

Some oligosaccharides are regarded as biological constituents with benefits to human health in an indirect way. They enter the intestinal tract to be fermented by the gut microbiota, causing changes in the abundance and composition of the gut microbiota and producing fermentation products such as short-chain fatty acids (SCFAs). In this review, the structural features and biological activities of eight common natural oligosaccharides were summarized, including human milk oligosaccharides (HMOS), xylo-oligosaccharides (XOS), arabinoxylo-oligosaccharides (AXOS), isomaltooligosaccharides (IMOS), chitin oligosaccharides (NACOS), mannan-oligosaccharides (MOS), galacto-oligosaccharides (GOS) and fructo-oligosaccharides (FOS).

Marine unsaturated fatty acids: structures, bioactivities, biosynthesis and benefits.

Unsaturated fatty acids (UFAs) are an important category of monounsaturated and polyunsaturated fatty acids with nutritional properties. These secondary metabolites have been obtained from multitudinous natural resources, including marine organisms. Because of the increasing numerous biological importance of these marine derived molecules, this review covers 147 marine originated UFAs reported from 1978 to 2018.

[Effect of Shaoyao Tang on ulcerative colitis in rats via regulation of TLR4/NF-κB signal pathway].

The aim of this paper was to investigate the effect of Shaoyao Tang on ulcerative colitis(UC) in rats via regulation of TLR4/NF-κB signal pathway. A total of 56 Wistar rats were randomly divided into 6 groups: normal control group(double distilled water), model group(double distilled water), mesalazine group(10 mL·kg~(-1)), high dose, middle dose and low dose Shaoyao Tang groups(2.4, 1.

Efficacy and safety of anti-amyloid- immunotherapy for Alzheimer's disease: a systematic review and network meta-analysis.

To review the optimality and safety of different anti-Amyloid-(Aβ) immunotherapies for Alzheimer's disease (AD). Published randomized controlled trials were comprehensively reviewed from electronic databases (Cochrane library, Embase, Pubmed, and Google scholar). Pooled outcomes as mean difference or odds ratio values with 95% confidence interval were reported.

Lung morphometry changes in prevention of airway remodeling by protocatechuic aldehyde in asthmatic mice.

Airway remodeling can lead to irreversible airflow obstruction and persistent airway hyper-responsiveness, which is the pathological basis of refractory asthma. To investigate the preventive effect of protocatechuic aldehyde on airway remodeling in asthmatic mice by lung morphometry methods. BALB/c mice were used to establish model of airway remodeling by ovalbumin (OVA) inhalation.