Results 51 to 60 of about 824,973 (281)

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

Direct Access to Chiral Piperidines by Enantioselective HAT‐Initiated C(sp3)─H Oxidation

Angewandte Chemie, EarlyView.
The direct desymmetrization of piperidines is achieved through manganese‐catalyzed enantioselective α‐C(sp3)─H oxidation with hydrogen peroxide, affording versatile chiral N,O‐acetals in good yields and with high enantio‐ and diastereoselectivity. These intermediates provide access to diverse functionalized piperidines with retention of chirality ...
Sethuraman Muthuramalingam, Josep M. Luis, Arnau Call, Quentin Lefebvre, Matthew S. Sigman, Miquel Costas   +5 more
wiley   +2 more sources

Asymmetric Single‐Atom Catalysts Govern Diffusible and Non‐Diffusible Non‐Radical Pathways for Selective Degradation of Antibiotic Resistance Genes

Advanced Science, EarlyView.
Asymmetric single‐atom metal‐nitrogen‐carbon catalysts modulate the non‐radical pathway during peroxymonosulfate (PMS) activation. A fundamental contrast was revealed between diffusible singlet oxygen (1O2) and non‐diffusible electron‐transfer pathways (ETP) in antibiotic resistance gene (ARG) degradation.
Chen Gao, Jun Sun, Liang Zhang, Litao Lin, Zongfeng Wan, Bingcai Pan, Sheng Tang   +6 more
wiley   +1 more source

Structural and Functional Siderophore Remodeling by Enzymatic Delipidation

Angewandte Chemie, EarlyView.
A surprising functional switch in bacterial siderophores was discovered through genome mining and the analysis of environmental and pathogenic Pandoraea species. Pandorachelin B, a lipocyclopeptide that promotes swarming motility, is cleaved by a specialized acylase, yielding a ring‐contracted, homodetic cyclopeptide, pandorachelin A, which exhibits ...
Elena Herzog, Keishi Ishida, Evelyn M. Molloy, Ron Hermenau, Kirstin Scherlach, Christian Hertweck   +5 more
wiley   +2 more sources

Mutations in beta-lactam resistance determining regions and beta lactam resistance profiles.

, 2018
Mutations in beta-lactam resistance determining regions and beta lactam resistance profiles.
Ajay Kumar Vijay (5802035), Gurjeet Singh Kohli (5802038), Scott A. Rice (143316), Dinesh Subedi (5802032), Mark Willcox (749527)   +4 more
core   +1 more source

Visible‐Light‐Mediated Lewis Acid‐Catalyzed Diradical Hydrogen Atom Transfer Reaction of Enamides

Advanced Science, EarlyView.
The Lewis acid catalysis was crucial for the success of the DHAT reaction of enamides by lowering the energy of the triplet excited state and modulating the reactivity of the formed diradical intermediate in a carbon‐to‐carbon 1,5‐DHAT and consequent cyclization that allows the functionalization of C(sp3)−H bonds to construct a variety of novel β ...
Yao Huang, Baoyu Yang, Xiang Zhou, Israel Fernández, Kexue Xia, Yang Xiong   +5 more
wiley   +1 more source

Beyond Simple Mimicry: Next‐Generation Geometric Architectures and Future Paradigms in Small‐Molecule and Macrocyclic Peptidomimetics

Angewandte Chemie, EarlyView.
Peptide‐to‐Small Molecule Paradigm: Peptidomimetics have evolved from simple mimicry toward drug‐like scaffolds supported by increasing clinical successes. This Perspective highlights the geometric design principles—linear repetition, convergent fusion, and cyclization—defining the next‐generation peptidomimetic architectures capable of targeting ...
Jesang Lee, Sumin Son, Jeong Yeon Yoo, Ji Hyae Lee, Meehyun Chun, Seung Bum Park   +5 more
wiley   +2 more sources

Reorganization of Innate Immune Cell Lipid Profiles by Bioinspired Meroterpenoids to Limit Inflammation

Advanced Science, EarlyView.
Resolution pharmacology is an emerging strategy to tackle inflammatory pathologies. Bioinspired meroterpenoids induce a lipid mediator class switch toward inflammation resolution in vitro and in vivo by targeting key nodes in lipid mediator biosynthesis and neutral lipid dynamics.
Lorenz Waltl, David Holubek, Klaus Speck, Raphael Wildermuth, Franz‐Lucas Haut, Stephan Permann, Immanuel Plangger, Christian Steinborn, Zhigang Rao, Danilo D'Avino, Ida Cerqua, Julia Stadler, Fiorentina Roviezzo, Peter Schlenke, Anita Siller, Harald Schennach, Solveigh C. Koeberle, Eva‐Maria Pferschy‐Wenzig, Antonietta Rossi, Thomas Magauer, Andreas Koeberle   +20 more
wiley   +1 more source

Intramolecular Nickel‐Catalyzed Reductive Coupling: Enantioselective Synthesis of Tetrahydroisoquinolines and Related Heterocycles

Angewandte Chemie, EarlyView.
The successful extension of the nickel‐catalyzed asymmetric coupling of polarized 1,3‐dienes with aldehydes to an intramolecular setting opens an efficient new entry into hydroxylated N‐heterocyclic compounds, most notably valuable tetrahydroisoquinolines.
Thilo Bender, Markus Leutzsch, Yannik Sell, Alois Fürstner   +3 more
wiley   +2 more sources

Comparison of Effectiveness between Combination of Beta-Lactam with Azyhtromycin or Levofloxacin for Adult Pneumonia Patients

Pharmacology and Clinical Pharmacy Research, 2018
Treatment for pneumonia has always been a challenge due to the difficulties in diagnosis and the growing incidence of antibiotic resistance. Beta-lactam antibiotics are the first line treatment for pneumonia.
Gina Arifah, Eli Halimah, Rizky Abdulah
doaj   +1 more source