[structure: see text] Single enantiomer, chiral donor-acceptor metal complexes were synthesized via the self-discriminating zinc(II) complexation of a pseudoracemic mixture of donor/acceptor-substituted bisoxazoline derivatives.
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http://dx.doi.org/10.1021/ol060836s | DOI Listing |
Int J Mol Sci
December 2024
Department of Chemistry and Biochemistry, Loyola University Chicago, 1032 West Sheridan Road, Chicago, IL 60660, USA.
Based on the inhibitory potencies from earlier reported tetrazole thioether analogs, we now describe the synthesis and inhibition of pyrazole-based inhibitors of -succinyl-l,l-2,6-diaminopimelic acid desuccinylase (DapE) from (DapE). The most potent pyrazole analog bears an aminopyridine amide with an IC of 17.9 ± 8.
View Article and Find Full Text PDFJ Am Chem Soc
December 2024
School of Natural Sciences, Department Chemie, and Catalysis Research Center (CRC), Technische Universität München, Lichtenbergstrasse 4, 85747 Garching, Germany.
By coupling a photochemical and a thermal step, a single chiral catalyst can establish a photostationary state in which the enantiopure form of a chiral compound is favored over its racemate. Following this strategy, 3-substituted 4,7-diaza-1-isoindolones were successfully deracemized (74-98% yield, 86-99% ) employing 2.5 mol % of a photocatalyst.
View Article and Find Full Text PDFJ Colloid Interface Sci
December 2024
School of Health Sciences, Stopford Building, The University of Manchester, Oxford Road, Manchester M13 9PT, UK.
Hypothesis: Nanoscale characterisation of the self-associated species formed by amphiphilic pharmaceuticals in aqueous solution carries relevance across their entire journey from development through to manufacture - relevant, therefore, not only as regards formulation of the drug products as medicines, but also potentially relevant to their bioavailability, activity, and clinical side effects. Such knowledge and understanding, however, can only be fully secured by applying a range of experimental and theoretical methodologies.
Experiments: Herein, we apply a synergistic combination of solubility, surface tension, SANS, NMR and UV spectroscopic studies, together with MD simulation and QM calculations, to investigate the meso-structures of propranolol hydrochloride aggregates in bulk aqueous solutions, at concentrations spanning 2.
Org Chem Front
December 2024
Department of Chemistry, University of Basel St Johanns-Ring 19 Basel 4056 Switzerland https://www.chemie1.unibas.ch/Bmayor/.
This work explores the use of a cross-shaped organic framework that is used as a template for the investigation of multi-functionalized chromophores. We report the design and synthesis of a universal cross-shaped building block bearing two bromines and two iodines on its peripheral positions. The template can be synthesized on a gram scale in a five-step reaction comprising an oxidative homo-coupling macro-cyclization.
View Article and Find Full Text PDFProg Neuropsychopharmacol Biol Psychiatry
December 2024
Chiba University Center for Forensic Mental Health, Chiba 260-8670, Japan; Department of Anesthesiology, Pain and Perioperative Medicine, The First Affiliated Hospital of Zhengzhou University, Zhengzhou 450052, China. Electronic address:
Postoperative cognitive dysfunction (POCD) is characterized by a decline in cognitive functions, including memory, attention, and executive abilities, following surgery, with no effective therapeutic drugs currently available. Arketamine, the (R)-enantiomer of ketamine, has shown promise in mitigating cognitive deficits in animal models. In this study, we investigated whether arketamine could ameliorate cognitive deficits in a mouse model of POCD, with a focus on the role of transforming growth factor (TGF)-β1 in its effects.
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