[reaction: see text] Reaction of carbamoyl chlorides with cyano-Gilman cuprates affords tertiary amides in good to excellent yields. The reaction is general due to the possibility of using reagents made either from organolithium or from Grignard compounds. The characterization of the main side products allowed for the suggestion of a possible mechanism.
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http://dx.doi.org/10.1021/ol0487130 | DOI Listing |
Mol Biol Rep
January 2025
Department of Biomedical Laboratory Science and Management, Vidyasagar University, Midnapore, West Bengal, 721102, India.
Background: Rising antimicrobial resistance (AMR) is an acute public health emergency impeding the clinical efficacy of surgical interventions. Biliary stent placement is one of the routine surgical procedures that rarely lead to infections that are empirically managed by broad-spectrum β-lactams and fluoroquinolones. Critical priority pathogens, such as carbapenem-resistant Escherichia coli challenge treatment outcomes and infection prevention.
View Article and Find Full Text PDFOrg Lett
January 2025
Pingyuan Laboratory, School of Chemistry and Chemical Engineering, Henan Normal University, Xinxiang, Henan 453007, People's Republic of China.
An asymmetric photoredox catalytic Minisci-type reaction between α-bromide amides and imine-containing azaarenes has been successfully developed. This catalyst system employs a chiral phosphoric acid alongside 3DPAFIPN as a photosensitizer. The reaction produces a diverse array of valuable amides, featuring azaarene-substituted tertiary carbon stereocenters at the β-position, in high yields (up to 85%) and good to excellent enantioselectivities (up to >99% enantiomeric excess (ee)).
View Article and Find Full Text PDFBiochemistry
January 2025
Division of Clinical Pharmacology, Indiana University School of Medicine, Indianapolis, Indiana 46202, United States.
In the wake of the pandemic, peptidyl protease inhibitors with Pro-based rigid Leu mimetics at the P position have emerged as potent drug candidates against the SARS-CoV-2 main protease. This success is intuitively attributed to the enhanced hydrophobic interactions and rigidity of Pro-based rigid Leu mimetics in the literature. However, the tertiary amide of proline P derivatives, which hinders the formation of a critical hydrogen bond with the enzyme active site, and the constrained PP conformation, which contradicts the protease preferred β-strand conformation, represent two overlooked disadvantages associated with these inhibitors over traditional inhibitors and, theoretically, should adversely affect their potency.
View Article and Find Full Text PDFBMJ Open
December 2024
Department of Anesthesiology, Peking University First Hospital, Beijing, China
Objective: To investigate the impact of dexmedetomidine-ropivacaine combination versus sufentanil-ropivacaine combination for epidural labour analgesia on neonatal and maternal outcomes and test the feasibility of a future large, randomised trial.
Design: A randomised, double-blind, pilot clinical trial from 16 March 2023 to 15 June 2023.
Setting: A tertiary-care hospital in Beijing, China.
Pathogens
December 2024
Department of Internal Medicine, University Hospital of Patras, 265 04 Patras, Greece.
: The increased prevalence of antibiotic resistance among Gram-negative bacteria presents a severe public health challenge, leading to increased mortality rates, prolonged hospital stays, and higher medical costs. In Greece, the issue of multidrug-resistant Gram-negative bacteria is particularly alarming, exacerbated by overuse of antibiotics and inadequate infection control measures. This study aimed to detect the prevalence of extensively drug-resistant (XDR) Gram-negative bacteria in a tertiary hospital in Western Greece over the last eight years from 2016 to 2023.
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