Chengyuan Liang

3D Electron Diffraction Elucidates the Structure of a 1,3,5-Triazin-2,4-dione Cinnamamide Covalent Inhibitor of SARS-CoV-2 3CLpro

Ge Meng, Peizhi Yan, Boxin Zhang, Bingxing Zhang et autres

Abstract The coronavirus 3-chymotrypsin-like protease (3CLpro) is an essential target for anticoronavirus drug discovery. Eleven covalent 1,3,5-triazin-2,4-dione cinnamamides (1a–1k) bearing a Cys145-directed α,β-unsaturated Michael acceptor were synthesized and evaluated against SARS-CoV-2 3CLpro. 1a showed the highest potency (IC50 = 92.45 nM) and …

cn (code pays fourni par la source)

Oral Small-Molecule GLP-1 Receptor Agonists: Lessons from Clinical Candidates and a Blueprint for Next-Generation Design

Jinrong Hu, Yunfei Zhang, Mengzhou Wang, Boxin Zhang et autres

Abstract Glucagon-like peptide-1 receptor agonists (GLP-1RAs) have revolutionized the treatment of type 2 diabetes (T2D) and obesity, yet all approved therapies to date are peptidic, limiting dosing convenience and patient acceptance. The recent clinical advancement of oral, nonpeptidic GLP-1 RAs, including danuglipron, …

cn, us (code pays fourni par la source)

Phytocannabinoid Cannabidiol (CBD) in Neurodegenerative Diseases: From Polypharmacology to Drug Development

Bingxing Zhang, Jiang Nan, Yunfei Zhang, Boxin Zhang et autres

cn (code pays fourni par la source)

Six-Membered N-ANP-Enabled Tandem Catellani/Buchwald Annulation for the Construction of π-Extended Dibenzocarbazoles

Xue Gong, Lei Tian, S Liu, Chengyuan Liang et autres

We report a Pd/NBE/Cu-catalyzed tandem Catellani/Buchwald annulation for the direct C–H/N–H [3+4] cyclization of carbazoles with aryl iodonium salts. This protocol provides efficient access to a range of π-extended dibenzocarbazole frameworks with broad substrate applicability. The reaction operates through a challenging six-membered …

cn (code pays fourni par la source)

Echinacoside restores levofloxacin activity against multidrug-resistant Pseudomonas aeruginosa: evidence for iron-responsive siderophore-like properties and membrane disruption

Lei Tian, Y Zhang, Boxin Zhang, Jinrong Hu et autres

cn (code pays fourni par la source)

Respiratory Syncytial Virus (RSV) Small-Molecule Therapeutics Sail Between Scylla and Charybdis Toward Clinical Breakthroughs

Lei Tian, Sundian Liu, Boxin Zhang, Jinrong Hu et autres

ABSTRACT The recurrent morbidity of respiratory syncytial virus (RSV) in infants and older adults underscores the need for accelerated antiviral discovery. However, no small-molecule therapeutics have received approval. This review systematically evaluates two decades of structure-activity relationships, druggability assessments, and clinical outcomes. …

cn (code pays fourni par la source)

Dual-mode sensor array based on silica-coated carbon dots with tunable fluorescence and phosphorescence for discrimination and detection of monoamine neurotransmitters

Yongbo Wang, Yuanna Ning, Shaojie Wang, Wencai Wang et autres

cn (code pays fourni par la source)

Conformationally restricted pleuromutilins via a pyridinyl-amide tether bias peptidyl transferase center engagement enabling broad-spectrum potency against multidrug-resistant bacteria

Lansheng Zhang, Bingxing Zhang, Lei Tian, Juan Xia et autres

cn (code pays fourni par la source)

List of contributors

Tanvir Ahmed, Ahmed A. Al-Karmalawy, Feifei An, Ömer Aras et autres

bd, iq, Égypte, cn, us, in, ir, be (code pays fourni par la source)

Danuglipron: pioneering oral glucagon-like peptide-1 receptor agonists paving the way forrevolutionizing diabetes treatment

Jinrong Hu, Ying Zhou, J. Li, Lei Tian et autres

Remdesivir: an early repurposed RNA-dependent RNA polymerase inhibitor for treating COVID-19

Lei Tian, Jiayun Zhang, Boxin Zhang, Xiuding Yang et autres

cn (code pays fourni par la source)

Particle size-dependent antibacterial activity of emodin nanocrystals against Staphylococcus aureus

Bin Tian, Weijia Wang, Hui Chen, Xuezhi Zhuo et autres

cn (code pays fourni par la source)