Results 81 to 90 of about 74,505 (292)

In vitro and in vivo activity of d-serine in combination with β-lactam antibiotics against methicillin-resistant Staphylococcus aureus

Acta Pharmaceutica Sinica B, 2019
As d-amino acids play important roles in the physiological metabolism of bacteria, combination of d-amino acids with antibiotics may provide synergistic antibacterial activity.
Qing Wang, Yuemeng Lv, Jing Pang, Xue Li, Xi Lu, Xiukun Wang, Xinxin Hu, Tongying Nie, Xinyi Yang, Yan Q. Xiong, Jiandong Jiang, Congran Li, Xuefu You   +12 more
doaj   +1 more source

Spiro-Lactams as Novel Antimicrobial Agents

, 2020
Introduction: Structural modulation of previously identified lead spiro-β-lactams with antimicrobial activity was carried out. Objective: The main objective of this work was to synthesize and evaluate the biological activity of novel spiro-lactams ...
Bártolo, Inês, Fontinha, Diana, Esteves, Margarida I. M., Melo, Teresa M. V. D. Pinho e, Soares, Maria I. L., Caratão, Cátia C., Alves, Nuno G., Alves, Américo J. S., Lopes, Susana M. M., Prudêncio, Miguel, Taveira, Nuno   +10 more
core   +1 more source

Structural Basis of Shiga Toxin Neutralization by Human Antibodies Targeting Canonical Receptor‐Binding and Non‐Canonical Assembly Sites

Advanced Science, EarlyView.
Cryo‐electron microscopy structures reveal two distinct neutralization mechanisms of fully human monoclonal antibodies targeting the Shiga toxin 1a B subunit. RDS059 occludes the Gb3 receptor‐binding site, whereas RDS045 engages a lateral quaternary epitope to disrupt holotoxin assembly.
Jianting Ke, Xin Li, Xiaoli Wang, Zhaoxia Huang, Shaojie Xue, Yuyang Liu, Jing Pan, Guowei Hu, Yayu Wang, Cheng Wang, Shoudeng Chen   +10 more
wiley   +1 more source

Macrocyclization of ω‐Isocyano Aldehydes

Angewandte Chemie, EarlyView.
The ω‐isocyano aldehydes readily undergo cyclization to afford α‐acyloxy, α‐hydroxy, α‐acetamido, and α‐keto macrolactams, as well as tetrazole‐fused macrocycles, via C(sp3)─C(sp2) bond formation, providing access to diverse α‐functionalized medium‐sized lactams and macrolactams. ABSTRACT Medium‐sized rings and macrocycles constitute a privileged class
Baochao Yang, Teerawat Songsichan, Cyril Piemontesi, Qian Wang, Jieping Zhu   +4 more
wiley   +2 more sources

Eosin Y- and Copper-Catalyzed Dark Reaction To Construct Ene-γ-Lactams

, 2018
Eosin Y, a common organo-photocatalyst in visible-light photoredox processes, was found to show excellent catalytic activities for thermal redox reactions under a catalytic amount of Cu­(OAc)2.
Kai-Wen Feng (4534645), Wen-Long Lei, Tao Wang, Qiang Liu (166143), Qiang Liu, Tao Wang (12008), Wen-Long Lei (4534648), Kai-Wen Feng, Li-Zhu Wu (654284), Li-Zhu Wu   +9 more
core   +1 more source

Photoinduced Temperature-Regulated Selective Carbene C–H Insertion for the Synthesis of Functionalized Spiro-β-lactones and -lactams

, 2023
A temperature-regulated catalyst-free photoinduced selective carbene C–H insertion strategy was realized to efficiently synthesize spiro-β-lactones and -lactams, which hold considerable promise in drug discovery programs.
Durga Prasad Hari, Bhismalochan Ghorai, Abdur Rouf Samim Mondal, Bhismalochan Ghorai (16269898), Durga Prasad Hari (1344915), Abdur Rouf Samim Mondal (16269895)   +5 more
core   +1 more source

Predicting Enzyme Turnover Numbers and Enabling Rational Enzyme Evolution

Advanced Science, EarlyView.
MCKcat, a deep learning framework combining multi‐scale convolution and cross‐attention, accurately predicts enzyme turnover number (kcat) by fusing sequence and reaction representations. It couples with rational design in a two‐step strategy for Bacillus aryabhattai laccase engineering, achieving a 75% positive rate with synergistically enhanced ...
Fengya Ge, Xiangyang Ma, Jiyan Li, Mengxiang Wang, Fuping Lu, Yihan Liu, Lin Wang   +6 more
wiley   +1 more source

Rational Design of a Synthetic Galliphore for the Diagnostic Nuclear Imaging and Treatment of Bacterial Infections

Angewandte Chemie, EarlyView.
KO‐NH2 is a synthetic metallophore that preferentially binds Ga3+ over Fe3+ and is recognized by bacterial transporters. Photocrosslinking identifies CirA and Fiu as key uptake proteins in E. coli. KO‐NH2 enables targeted imaging and treatment of E. coli soft tissue infections.
Phuong Nguyen Tran, Axia Marlin, Edith K. Amason, Marie Huynh, Hannah Carlisle, Eszter Boros   +5 more
wiley   +2 more sources

Cobalt-Catalyzed One-Pot Three-Component Coupling Route to β-Acetamido Carbonyl Compounds:  A General Synthetic Protocol for γ-Lactams

, 2016
An efficient improved procedure for the synthesis of β-acetamido carbonyl compounds is developed by a cobalt(II) chloride-catalyzed three-component coupling protocol.
Javed Iqbal (2121922), I. Nageshwar Rao (3032109), Saibal Kumar Das (3032112), E. N. Prabhakaran (3031473)   +3 more
core   +1 more source

Penicillin‐binding protein PBP2a provides variable levels of protection toward different β‐lactams in Staphylococcus aureus RN4220

MicrobiologyOpen, 2020
Methicillin‐resistant Staphylococcus aureus (MRSA) is resistant to most β‐lactams due to the expression of an extra penicillin‐binding protein, PBP2a, with low β‐lactam affinity.
Marte Ekeland Fergestad, Gro Anita Stamsås, Danae Morales Angeles, Zhian Salehian, Yngvild Wasteson, Morten Kjos   +5 more
doaj   +1 more source