Results 61 to 70 of about 56,729 (249)

Targeted Degradation of Picornaviral 3C Protease via PROTACs Confers High Barrier to Viral Resistance and Broad‐Spectrum Antiviral Activity

Advanced Science, EarlyView.
This study reports D34 as the first PROTAC degrader that targets the 3C protease of picornaviruses. D34 effectively degrades EV71 3C protease via the ubiquitin‐proteasome pathway. More importantly, D34 exhibits a high resistance barrier and shows broad‐spectrum antiviral activity against multiple picornaviruses, highlighting its potential as a novel ...
Weilong Deng, Junyu Chen, Yingyue Pang, Yuanyuan Zhang, Siqian Chen, Guoliang You, Xiaoman Tian, Zhongxin Xu, Jing Wang, Luqing Shang   +9 more
wiley   +1 more source

Iridium‐Catalyzed Ionic Hydrogenation of Multi‐Aza Heterocycles

Angewandte Chemie, EarlyView.
Saturated nitrogen‐containing heterocycles are ubiquitous in bioactive molecules and are thus attractive synthetic targets. A readily accessible cyclometalated iridium(III) complex reduces 14 different aromatic aza heterocycles to (partially)saturated multi aza‐heterocycles enlarging accessible chemical space while displaying high tolerance toward ...
Arthur Despois, Nicolai Cramer
wiley   +2 more sources

Combatting Pseudomonas aeruginosa with β-Lactam Antibiotics: A Revived Weapon?

Antibiotics
Pseudomonas aeruginosa is a significant threat to public health as an aggressive, opportunistic pathogen. The use of β-lactam antibiotics such as penicillins, cephalosporins, monobactams, and carbapenems remains a front-line treatment against P ...
Dylan W. Zhao, Christopher T. Lohans
doaj   +1 more source

High‐Density E. Coli Cultivation Arrays for Combinatorial Drug Testing With Subsequent Lipid Profiling by MALDI‐MS

Advanced Science, EarlyView.
High‐throughput antibiotic cross‐gradient assays on microdroplet arrays. A multichannel printhead together with five pressure regulators forms droplet arrays of up to 20 832 droplets within 25 minutes. Each droplet contains unique concentrations of antibiotics, allowing to moniture a vast spectrum of bacterial repsonses over night. The bacterial growth
M. Breitfeld, C. L. Dietsche, F‐L. Born, I. Onipko, L. Blaase, P. S. Dittrich   +5 more
wiley   +1 more source

Photochemical Ring Opening of Cyclopropyl Silyl Ethers Enables β–β Coupling, Radical‐Polar Crossover and Annulation

Angewandte Chemie, EarlyView.
A photochemical platform enables β–β coupling of cyclopropyl silyl ethers with electron‐deficient alkenes. The resulting adducts serve as entry points into annulative and radical–polar crossover pathways, providing rapid access to fused, bridged, and spirocyclic architectures, including late‐stage scaffold diversification to diterpene‐like carbocyclic ...
Jacop Rydén, Eilidh Young, Wilma Olsson, Eskil Flodén, Mattias Tan, Sebastian Clementson   +5 more
wiley   +2 more sources

A novel method to depurate β-lactam antibiotic residues by administration of a broad-spectrum β-lactamase enzyme in fish tissues

Fisheries and Aquatic Sciences, 2016
As a novel strategy to remove β-lactam antibiotic residues from fish tissues, utilization of β-lactamase, enzyme that normally degrades β-lactam structure-containing drugs, was explored.
Young-Sik Choe, Ji-Hoon Lee, Soo-Geun Jo, Kwan Ha Park   +3 more
doaj   +1 more source

Pyrazole‐Derived Antibacterial Compounds Effectively Treat Methicillin‐Resistant Staphylococcus Aureus Infections by Inhibiting Aspartate Transcarbamoylase

Advanced Science, EarlyView.
This study unveils a novel antibacterial mechanism against MRSA, in which the compound Py‐27 selectively targets and inhibits aspartate transcarbamoylase (ATCase), a key enzyme in pyrimidine synthesis. This inhibition disrupts DNA replication, induces oxidative damage, leading to potent bactericidal activity.
Xiaorong Yang, Xinyuan Cao, Lixia Dai, Feng Yang, Jing Wang, Yudong Ma, Tong Bu, Zile Gong, Xueyan Liu, Changcai Bai, Xiaolou Miao, Xiaofei Shang   +11 more
wiley   +1 more source

Borylcyclopropanes: Synthetic Strategies and Applications

Angewandte Chemie, EarlyView.
Borylcyclopropanes (cyclopropanes bearing a boron substituent) sit at the intersection of two privileged frameworks in synthesis. This review provides the first exhaustive survey of their chemistry, spanning metal–carbene, nucleophilic cyclization, radical, hydroboration, and C─H activation routes, and documenting applications in medicinal chemistry ...
Aiza A. Butt, Joseph M. Ready
wiley   +2 more sources

Synthetic Lethality Reveals Mechanisms of Mycobacterium tuberculosis Resistance to β-Lactams

mBio, 2014
Most β-lactam antibiotics are ineffective against Mycobacterium tuberculosis due to the microbe’s innate resistance. The emergence of multidrug-resistant (MDR) and extensively drug-resistant (XDR) strains has prompted interest to repurpose this class of ...
Shichun Lun, David Miranda, Andre Kubler, Haidan Guo, Mariama C. Maiga, Kathryn Winglee, Shaaretha Pelly, William R. Bishai   +7 more
doaj   +1 more source

Teicoplanin versus β-lactam for febrile patients with Staphylococcus-like bacteremia: focus on methicillin-susceptible Staphylococcus aureus bacteremia

BMC Infectious Diseases, 2021
Background Many studies have shown that vancomycin is inferior to β-lactam antibiotics in terms of effectiveness in the treatment of methicillin-susceptible Staphylococcus aureus (MSSA) bacteremia.
Ching-Yen Tsai, Chen-Hsiang Lee, I-Ling Chen   +2 more
doaj   +1 more source