Results 51 to 60 of about 764,478 (294)

Natural Products Inspired Scaffold Diversification Leads to Unnatural Molecular Warhead and Covalent Strategy to Modulating Protein Function through Electrophilic Bromine Transfer

Advanced Science, EarlyView.
We report a new thiolate‐reactive α,α‐gem‐dibromo lactam warhead that activates transcription factor Nrf2 and demonstrates anti‐inflammatory activities, which have implications in cancer, neurodegeneration, and cardiovascular diseases. RNA‐seq illuminated detailed transcriptional profiles, and chemical reactions with cysteine‐containing compounds ...
Beau R. Brummel, Sofia Kokkaliari, Qiwen Gao, Jinjing Chen, Larissa Costa de Almeida, Srinivasarao Tenneti, Derek A. Leas, Eli Levit, Lewis S. Alexander, Khalil A. Abboud, Pingrong Wei, Michael D. Cameron, James R. Rocca, Ranjala Ratnayake, Donna D. Zhang, Hendrik Luesch, Robert W. Huigens III   +16 more
wiley   +1 more source

Activity of OP0595/β-lactam combinations against Gram-negative bacteria with extended-spectrum, AmpC and carbapenem-hydrolysing β-lactamases [PDF]

Journal of Antimicrobial Chemotherapy, 2015
OP0595 is a diazabicyclooctane that (i) acts as a PBP2-active antibacterial, (ii) inhibits Class A and C β-lactamases and (iii), like mecillinam, gives β-lactamase-independent potentiation of β-lactams targeting other PBPs. We tested its behaviour against β-lactam-resistant Enterobacteriaceae and non-fermenters.Organisms were UK clinical isolates; MICs
Livermore, David M., Mushtaq, Shazad, Warner, Marina, Woodford, Neil   +3 more
openaire   +4 more sources

Diversity of Pharmaceuticals Enhances Antibiotic Resistance in the Invertebrate Gut via Biofilm‐Mediated Mechanisms

Advanced Science, EarlyView.
Pharmaceutical diversity acts as an independent driver of antibiotic resistance in soil invertebrates. While bulk soil remains unaffected, the collembolan gut microbiome exhibits significant resistance gene enrichment under complex chemical exposure and diurnal warming.
Yi‐Fei Wang, Ya‐Ning Wang, Da Lin, Jia‐Yang Xu, Feng‐Yuan Qi, Hui‐Ling Cui, Hui‐Jie Lu, Min Qiao, Edward Topp, Dong Zhu, Matthias C. Rillig, Yong‐Guan Zhu   +11 more
wiley   +1 more source

Catalytic Functionalization of Unactivated π‐Bonds Enabled by Bidentate Directing Auxiliaries

Angewandte Chemie, EarlyView.
This review explores how bidentate directing auxiliaries have advanced transition‐metal catalysis for unactivated alkene/alkyne functionalization. By leveraging chelated intermediates, bidentate directing auxiliaries enable precise hydrofunctionalization, difunctionalization, and C─H activation of π‐bonds with unique selectivity and reactivity.
Seunghyeon Cho, Al Vicente Riano D. Lisboa, Juntao Sun, Taeho Kang, Keary M. Engle   +4 more
wiley   +2 more sources

Neo-antigens for the serological diagnosis of IgE-mediated drug allergic reactions to antibiotics cephalosporin, carbapenem and monobactam

Scientific Reports, 2020
New antigens deriving from -lloyl and -llanyl, major and minor determinants, respectively, were produced for β-lactam antibiotics cefuroxime, cefotaxime, ceftriaxone, meropenem and aztreonam.
Edurne Peña-Mendizabal, Sergi Morais, Ángel Maquieira   +2 more
doaj   +1 more source

Substitution of Thr for Ala-237 in TEM-17, TEM-12 and TEM-26: alterations in β-lactam resistance conferred onEscherichia coli [PDF]

FEMS Microbiology Letters, 2001
Non-naturally occurring mutants of TEM-17 (E104K), TEM-12 (R164S) and TEM-26 (E104K:R164S) extended-spectrum (ES) beta-lactamases bearing threonine at position 237 were constructed by site-specific mutagenesis and expressed under isogenic conditions in Escherichia coli.
Giakkoupi, P., Hujer, A.M., Miriagou, V., Tzelepi, E., Bonomo, R.A., Tzouvelekis, L.S.   +5 more
openaire   +4 more sources

Stress History Establishes a Transient Tolerant State That Shapes Antibiotic Survival Upon Resuscitation

Advanced Science, EarlyView.
High‐throughput single‐cell analysis of resuscitating bacteria reveals a starvation‐history‐dependent transiently tolerant subpopulation that survives β$\beta$‐lactam exposure by temporarily reducing growth. Distinct from classical persisters, these actively growing yet dynamically modulated cells dominate survival across clinically relevant antibiotic
Kieran Abbott, Georgeos Hardo, Ruizhe Li, Jack Bradley, Ashraf Zarkan, Somenath Bakshi   +5 more
wiley   +1 more source

Catalytic Enantioselective Intramolecular Aza‐Michael Addition to α,β‐Unsaturated Esters

Angewandte Chemie, EarlyView.
A general method for accessing enantioenriched saturated N‐heterocycles via a catalytic enantioselective intramolecular aza‐Michael reaction to α,β‐unsaturated esters is described. A superbasic bifunctional iminophosphorane (BIMP) catalyst was key to enabling reactivity of the high pKa sulfonamide pronucleophile, whilst delivering good to excellent ...
Evan G. W. Rutter, Cameron J. MacRae, Haoran Xiong, Daniel Rozsar, Katherine F. P. Clarke, Darren J. Dixon   +5 more
wiley   +2 more sources

Chirality-Driven Folding of Short β‑Lactam Pseudopeptides

, 2016
Novel enantiopure pseudopeptide models containing a central -(β-lactam)-(Aa)- scaffold characterized by the combined presence of an α-alkyl-α-amino-β-lactam (i+1) residue and a α-substituted (i + 2) amino acid have been readily synthesized from α-alkyl ...
Claudio Palomo (1699948), Elena Andreieff (2001319), Eva Balentová (2001316), José Ignacio Miranda (2001325), Anthony Linden (1673590), Maialen Sagartzazu-Aizpurua (1397350), Jesus M. Aizpurua (1397347), Azucena Jimenez (2001322)   +7 more
core   +5 more sources

Comparison of initial empirical antibiotic regimens in severe community-acquired pneumonia: a network meta-analysis

BMC Pulmonary Medicine
Background Severe community-acquired pneumonia (SCAP) remains a leading cause of morbidity and mortality worldwide. Identifying the optimal antibiotic regimen for treating SCAP is crucial for improving patient outcomes.
Min Wang, Jing Zhang, Xiaoming Wang, Qian Wang, Lian Wang, Han Zhuang, Ao Liu   +6 more
doaj   +1 more source