Synthesis and Antiosteoporotic Characterization of Diselenyl Maleimides: Discovery of a Potent Agent for the Treatment of Osteoporosis by Targeting RANKL.

To discover new osteoclast-targeting antiosteoporosis agents, we identified forty-six diselenyl maleimides, which were efficiently prepared using a novel, simple, and metal-free method at room temperature in a short reaction time. Among them, showed the most marked inhibition of osteoclast differentiation with an value of 0.36 ± 0.

CircHIPK2 Contributes Cell Growth in Intestinal Epithelial of Colitis and Colorectal Cancer through Promoting TAZ Translation.

Colorectal cancer (CRC) and inflammatory bowel disease (IBD) are escalating global health concerns. Despite their distinct clinical presentations, both disorders share intricate genetic and molecular interactions. The Hippo signaling pathway plays a crucial role in regulating cell processes and is implicated in the pathogenesis of IBD and CRC.

Design, synthesis and biological evaluation of indoline-maleimide conjugates as potential antitumor agents for the treatment of colorectal cancer.

An efficient protocol for direct coupling of maleimides and indolines at the C7-position was achieved under Rh(III) catalysis. Thirty four novel indoline-maleimide conjugates were prepared in good to excellent yields using this method. All compounds were evaluated for their anti-proliferative effect against colorectal cell lines.

Design, Synthesis, and Biological Evaluation of β-Trifluoroethoxydimethyl Selenides as Potent Antiosteoporosis Agents.

An efficient protocol for the synthesis of β-trifluoroethoxydimethyl selenides was achieved under mild reaction conditions, and 39 compounds were prepared. All compounds were evaluated for their abilities to inhibit RANKL-induced osteoclastogenesis, compound exhibited the most potent activity. Further investigations revealed that could inhibit F-actin ring generation, bone resorption, and osteoclast-specific gene expression .

Metal-Free Radical [3 + 2] Annulation of Tetraalkylthiuram Disulfide with Alkynes/Alkenes: An Approach of Synthesizing 1,3-Dithiole and 1,3-Ditholane Derivatives.

A novel and metal-free [3 + 2] annulation of tetraalkylthiuram disulfide with alkynes/alkenes has been developed using Selectfluor at room temperature. The formed 1,3-dithiol-2-ylium/1,3-dithiolan-2-ylium salts can be easily transformed into the corresponding 1,3-dithiol-2-ylidenes/1,3-ditholan-2-ylidenes by one-pot subsequent condensation with malononitrile. The present protocol features the use of easily accessible starting materials, mild reaction conditions, good tolerance with diverse functional groups, easy scale-up, and a wide substrate scope, affording the desired products in good yields.

3-methyl-1H-indol-1-yl dimethylcarbamodithioate attenuates periodontitis through targeting MAPK signaling pathway-regulated mitochondrial function.

Periodontitis, the second most common oral disease, is primarily initiated by inflammatory responses and osteoclast differentiation, in which the MAPK signaling pathway and mitochondrial function play important roles. 3-methyl-1H-indol-1-yl dimethylcarbamodithioate (3o), a hybrid of indole and dithiocarbamate, was first synthesized by our group. It has shown anti-inflammatory activity against lipopolysaccharide-induced acute lung injury.

A novel small-molecule compound S-342-3 effectively inhibits the biofilm formation of .

Biofilms are an important virulence factor in and are characterized by a structured microbial community consisting of bacterial cells and a secreted extracellular polymeric matrix. Inhibition of biofilm formation is an effective measure to control infection. Here, we have synthesized a small molecule compound S-342-3, which exhibits potent inhibition of biofilm formation in both MRSA and MSSA.

Metal-Free Oxidative Dearomatization-Alkoxylation/Acyloxylation of Indoles: Synthesis of 2-Monosubstituted Indolin-3-ones.

A metal-free route for the preparation of 2-monosubstituted indolin-3-ones, including 2-alkoxyindolin-3-ones and 2-acyloxyindolin-3-ones from commercially available indoles, has been developed employing (bis(trifluoroacetoxy)iodo)benzene (PIFA) as an oxidant. The present protocol features mild reaction conditions, good tolerance with diverse functional groups, and a wide substrate scope, affording the desired products in good yields. This transformation is easy to scale up, and the desired products can be further modified.

Metal-Free Thiocarbamation of Quinolinones: Direct Access to 3,4-Difunctionalized Quinolines and Quinolinonyl Thiocarbamates at Room Temperature.

A novel and practical method for the preparation of difunctionalized quinolines, bearing a thiocarbamate group at the C3-position and an acyloxyl group at the C4-position, and quinolinonyl thiocarbamates from quinolinones, tetraalkylthiuram disulfides, and hypervalent iodine(III) reagents has been developed via thiocarbamation of quinolinones at room temperature. The present method features mild reaction conditions, good tolerance with diverse functional groups, and a wide substrate scope, providing the desired products in good yields. Furthermore, this transformation is easy to scale up, and the desired products can be readily converted to heterocyclic thiols.

Small-Molecule Compound CY-158-11 Inhibits Staphylococcus aureus Biofilm Formation.

Staphylococcus aureus is an important human pathogen and brings about many community-acquired, hospital-acquired, and biofilm-associated infections worldwide. It tends to form biofilms, triggering the release of toxins and initiating resistance mechanisms. As a result of the development of S.

C-H Diselenation and Monoselenation of Electron-Deficient Alkenes via Radical Coupling at Room Temperature.

A new, simple, and metal-free route for the diselenation of maleimides has been first developed employing (bis(trifluoroacetoxy)iodo)benzene (PIFA) at room temperature. The present method is compatible with different functional groups, and various diselenyl maleimides were obtained in moderate to excellent yields. Moreover, this protocol further highlights the unique practical application for the functionalization of biologically relevant molecules and amino acid derivatives.

Small-molecule compound SYG-180-2-2 attenuates virulence by inhibiting hemolysin and staphyloxanthin production.

Multi-drug resistant infection is still a serious threat to global health. Therefore, there is an urgent need to develop new antibacterial agents based on virulence factor therapy to overcome drug resistance. Previously, we synthesized SYG-180-2-2 (CHNOSe), an effective small molecule compound against biofilm.

Regioselective -C-H selenylation of aromatic compounds with weakly coordinating ketone groups.

A novel and versatile method for -C-H selenylation of aromatic compounds bearing ketone groups, including chromones, xanthones, acridinones, quinolinones and naphthoquinones with diselenides under Ru(II) catalysis is presented. Various chromones and diselenides are applicable for this transformation, affording 5-selenyl chromones in a highly regioselective manner in good to excellent yields. This transformation is easy to scale up and the desired products can be further modified.

Design, synthesis and biological evaluation of novel chromone-maleimide hybrids as potent anti-inflammatory agents against LPS-induced acute lung injury.

Acute lung injury (ALI) is an acute inflammatory disease, which severely impacts lung function with a high lethality rate. Chromone and maleimide are very important moieties of anti-inflammatory agents. Here, forty new chromone-maleimide hybrids were readily synthesized using a Heck-type coupling strategy in good yields and were screened for their anti-inflammatory activity.

Small-Molecule Compound SYG-180-2-2 to Effectively Prevent the Biofilm Formation of Methicillin-Resistant .

The resistance of methicillin-resistant (MRSA) has augmented due to the abuse of antibiotics, bringing about difficulties in the treatment of infection especially with the formation of biofilm. Thus, it is essential to develop antimicrobials. Here we synthesized a novel small-molecule compound, which we termed SYG-180-2-2 (CHNOSe), that had antibiofilm activity.

Chromone Derivatives CM3a Potently Eradicate Biofilms by Inhibiting Cell Adherence.

Introduction: The ability of to form biofilms is associated with high mortality and treatment costs. Established biofilms cannot be eradicated by many conventional antibiotics due to the development of antibiotic tolerance by . Here we report the synthesis and biological characterization of novel small-molecule compounds with antibiofilm activity.

The small molecule ZY-214-4 may reduce the virulence of Staphylococcus aureus by inhibiting pigment production.

Background: In recent years, clinical Staphylococcus aureus isolates have become highly resistant to antibiotics, which has raised concerns about the ability to control infections by these organisms. The aim of this study was to clarify the effect of a new small molecule, ZY-214-4 (CHBrNO), on S. aureus pigment production.

Antibiofilm Activity of Small-Molecule ZY-214-4 Against .

is the most important pathogenic bacteria in humans. As the resistance of to existing antibiotics is increasing, there is an urgent need for new anti-infective drugs. biofilms cause persistent infections and resist complete eradication with antibiotic therapy.

Ruthenium(II)-Catalyzed Direct C7-Selective Amidation of Indoles with Dioxazolones at Room Temperature.

A protocol for the preparation of 7-amido indoles via regioselective C-H bond functionalization has been first accomplished under Ru(II) catalysis. Indole derivatives and 4-aryl/heteroaryl/benzyl/alkyl dioxzaolines containing various substituents were applicable for this transformation, readily providing the amidated indoles in moderate to good yields. This novel process has many advantages, including good compatibility with diverse functional groups, broad substrate scopes, and mild reaction conditions.

Ruthenium(II)-Catalyzed C-H Activation of Chromones with Maleimides to Synthesize Succinimide/Maleimide-Containing Chromones.

An efficient route for the coupling of maleimides with chromones at the C5-position has been developed under Ru(II) catalysis. It could provide 1,4-addition products and oxidative Heck-type products by switching additives. Benzoic acid led to the formation of 1,4-addition products under solvent-free conditions, and silver acetate was promoted to the generation of oxidative Heck-type products.

Metal-free regioselective C-H chalcogenylation of coumarins/(hetero)arenes at ambient temperature.

A novel, practical and metal-free approach for the regioselective selenation of coumarins employing (bis(trifluoroacetoxy)iodo)benzene (PIFA) at room temperature is presented. The developed method is suitable for a wide substrate scope and affords 3-selenyl coumarins in good to excellent yields with high selectivity. A radical mechanism is proposed for this new transformation.

One-step construction of unsymmetrical thioureas and oxazolidinethiones from amines and carbon disulfide a cascade reaction sequence.

A concise and versatile method for the construction of unsymmetrical thioureas and oxazolidinethiones from amines and carbon disulfide has been achieved in DMSO without addition of extra reagents. The present protocol is compatible with various secondary amines and primary amines, and suitable for intermolecular and intramolecular reactions. Diverse unsymmetrical thioureas and oxazolidinethiones were efficiently obtained in good to excellent yields a cascade reaction sequence.

Base promoted synthesis of novel indole-dithiocarbamate compounds as potential anti-inflammatory therapeutic agents for treatment of acute lung injury.

An efficient protocol for highly chemoselective introduction of dithiocarbamate groups to nitrogen position of indoles with bis(dialkylaminethiocarbonyl)disulfides was achieved by employing t-BuOK as a promoter. Based on this methodology, twenty nine novel indole-dithiocarbamate compounds were prepared in moderate to excellent yields at room temperature. All compounds were evaluated for their anti-inflammatory activity.