Results 81 to 90 of about 38,167 (247)

Understanding the selectivity in the formation of δ-lactams vs. β-lactams in the Staudinger reactions of chloro-cyan-ketene with unsaturated imines. A DFT study† [PDF]

open access: yesRSC Advances, 2014
The reactions of chloro-cyan-ketene with two phenyl substituted unsaturated imines yielding β- or δ-lactams have been investigated using DFT methods at the MPWB1K/6-311G(d,p) level in diethyl ether.
Luis R. Domingo, José A. Sáez
doaj   +1 more source

Artificial Intelligence‐Guided Phenotypic Drug Repurposing Against Streptococcus pneumoniae

open access: yesAdvanced Science, EarlyView.
Integrated artificial intelligence (AI) ensembles identify highly potent repurposed drugs against Streptococcus pneumoniae. Prospective virtual screening of 6747 drugs uncovers nine active candidates, including thiostrepton. This drug exhibits low picomolar potency and bypasses established resistance in multidrug‐resistant strains, demonstrating an ...
Joshua S. Fitch   +6 more
wiley   +1 more source

Macrocyclization of ω‐Isocyano Aldehydes

open access: yesAngewandte 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   +4 more
wiley   +2 more sources

Combined dual β-lactams and diazabicyclooctane β-lactamase inhibitor is highly effective against Mycobacterium abscessus species in vitro

open access: yesJournal of Global Antimicrobial Resistance
Objective: Mycobacterium abscessus pulmonary disease is a refractory infectious disease. Developing an effective treatment is urgent as the number of patients infected with M. abscessus species (MABS) is increasing worldwide.
Kana Misawa   +8 more
doaj   +1 more source

In vitro activity of ceftolozane–tazobactam and ceftazidime–avibactam against clinical isolates of meropenem-non-susceptible Pseudomonas aeruginosa: A two-centre study

open access: yesJournal of Global Antimicrobial Resistance, 2020
Objectives: This study aimed to compare the activity of ceftazidime–avibactam (C/A), ceftolozane–tazobactam (C/T) and three anti-pseudomonal β-lactams (piperacillin–tazobactam, ceftazidime and cefepime) against a collection of meropenem-non-susceptible ...
Hasan Cenk Mirza   +6 more
doaj   +1 more source

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

open access: yesAdvanced 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   +10 more
wiley   +1 more source

Additional file 2: of Rapid antimicrobial susceptibility testing and β-lactam-induced cell morphology changes of Gram-negative biological threat pathogens by optical screening

open access: yes, 2018
Table S1. β-lactam-induced cell morphology changes in susceptible Burkholderia strains. (DOCX 22 kb)
McLaughlin, Heather, Sue, David
openaire   +1 more source

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

open access: yesAngewandte 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   +5 more
wiley   +2 more sources

Oral β-lactam combinations are effective in vitro against Mycobacterium avium, regardless of clarithromycin susceptibility

open access: yesMicrobiology Spectrum
The global incidence and prevalence of pulmonary disease caused by the Mycobacterium avium complex (MAC), mainly comprising M. avium and Mycobacterium intracellulare, is increasing.
Maiko Yoshikawa   +11 more
doaj   +1 more source

Predicting Enzyme Turnover Numbers and Enabling Rational Enzyme Evolution

open access: yesAdvanced 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   +6 more
wiley   +1 more source

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