New syntheses have been developed for the synthesis of (borohydrido-κ )tris-[η-(tri-methyl-sil-yl)cyclo-penta-dien-yl]uranium(IV), [U(BH)(CHSi)] or Cp'U(BH) (Cp' = CHSiMe) and its structure has been determined by single-crystal X-ray crystallography. This compound crystallized in the space group and the structure features three -coordinated Cp' rings and a -coordinated (BH) ligand.
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http://dx.doi.org/10.1107/S2056989021002425 | DOI Listing |
Acetyl CoA synthetases (ACS) have emerged as drug targets for the treatment of cancer, metabolic diseases as well as fungal and parasitic infections. Although a variety of small molecule ACS inhibitors have been discovered, the systematic optimization of these molecules has been slowed by a lack of structural information regarding their mechanism of inhibition. Through a chemical genetic-based, synthetic lethal screen of the human fungal pathogen Cryptococcus neoformans, we identified an isoxazole-based ACS inhibitor with antifungal activity and exquisite selectivity for the C.
View Article and Find Full Text PDFChem Commun (Camb)
January 2025
Institut für Anorganische Chemie, Eberhard Karls Universität Tübingen, Auf der Morgenstelle 18, D-72076 Tübingen, Germany.
The homoleptic complex La(InMe) is obtained from the respective aluminium congener La(AlMe) a donor-assisted tetramethylaluminate/tetramethylindate exchange protocol. Compound La(InMe) exhibits interesting thermal lability as well as distinct cluster formation like LaIn(C)(CH)(CH)(CH) and LaIn(CH)(CH) upon addition of an excess of donor or thermal treatment. The neutral potentially tridentate ligand MeTACN (1,4,7-trimethyl-1,4,7-triazacyclononane) is used to investigate donor-triggered intermediates.
View Article and Find Full Text PDFJ Microsc
January 2025
Department of Mechanical, Materials and Aerospace Engineering, University of Liverpool, Liverpool, UK.
Electron backscatter diffraction (EBSD) has developed over the last few decades into a valuable crystallographic characterisation method for a wide range of sample types. Despite these advances, issues such as the complexity of sample preparation, relatively slow acquisition, and damage in beam-sensitive samples, still limit the quantity and quality of interpretable data that can be obtained. To mitigate these issues, here we propose a method based on the subsampling of probe positions and subsequent reconstruction of an incomplete data set.
View Article and Find Full Text PDFAngew Chem Int Ed Engl
January 2025
Max-Planck-Institut fur Kohlenforschung, Organometallic Chemistry, Kaiser-Wilhelm-Platz 1, 45470, Mülheim/Ruhr, GERMANY.
Ynamides, when reacted with H2 or HBpin in the presence of [Cp*RuCl]4, convert into chiral-at-metal Fischer carbenes by regioselective gem-hydrogenation or gem-hydroboration of the polarized triple bond, respectively. gem-Hydroboration concomitantly affords a carbogenic borylated stereocenter adjacent to the ruthenium carbene unit, the configuration of which can be controlled using an Evans auxiliary. These are the first examples of asymmetric gem-addition reactions to alkynes known in the literature; representative pianostool ruthenium carbene complexes formed by this unconventional route were characterized by crystallographic and spectroscopic means.
View Article and Find Full Text PDFJ Med Chem
January 2025
Immunology Research Unit GlaxoSmithKline Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K.
Therapeutics promoting the endogenous production of IL-10 have the potential to restore homeostasis in inflammatory disorders such as inflammatory bowel disease (IBD). Here we describe the identification of a series of IL-10 upregulators based on a pyrimidyl-piperidine scaffold through a high throughput phenotypic CD4 T-cell multiplex assay. optimization of the initial hit yielded a lead with good potency and an clearance profile, compound 3-7, which additionally demonstrated efficacy in a murine endotoxin challenge PK-PD mechanistic model.
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