We present an expedient and economical route to a new spiroketal-based C -symmetric chiral scaffold, termed SPIROL. Based on this spirocyclic scaffold, several chiral ligands were generated. These ligands were successfully employed in an array of stereoselective transformations, including in iridium-catalyzed hydroarylations (up to 95 % ee), palladium-catalyzed allylic alkylations (up to 97 % ee), intermolecular palladium-catalyzed Heck couplings (up to 94 % ee), and rhodium-catalyzed dehydroalanine hydrogenation (up to 93 % ee).
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http://dx.doi.org/10.1002/anie.201713304 | DOI Listing |
Nat Chem
January 2025
State Key Laboratory of Inorganic Synthesis and Preparative Chemistry, Jilin University, Changchun, People's Republic of China.
Three-dimensional (3D) covalent organic frameworks (COFs) hold significant promise for a variety of applications. However, conventional design approaches using regular building blocks limit the structural diversity of 3D COFs. Here we design and synthesize two 3D COFs, designated as JUC-644 and JUC-645, through a methodology that relies on using eight-connected building blocks with reduced symmetry.
View Article and Find Full Text PDFSci Rep
January 2025
Professorship of Exercise Biology, Department Health and Sport Sciences, TUM School of Medicine and Health, Technical University of Munich, Munich, Germany.
While the effect of time-of-day (morning versus evening) on hormones, lipids and lipolysis has been studied in relation to meals and exercise, there are no studies that have investigated the effects of time-of-day on ice bath induced hormone and lipidome responses. In this crossover-designed study, a group of six women and six men, 26 ± 5 years old, 176 ± 7 cm tall, weighing 75 ± 10 kg, and a BMI of 23 ± 2 kg/mhad an ice bath (8-12 °C for 5 min) both in the morning and evening on separate days. Absence from intense physical exercise, nutrient intake and meal order was standardized in the 24 h prior the ice baths to account for confounders such as diet or exercise.
View Article and Find Full Text PDFAnticancer Agents Med Chem
January 2025
Department of Chemistry, Andhra University, Vishakapatnam, Andra Pradesh, India.
Background: Cancer presents a significant global health challenge, necessitating effective treatment strategies. While chemotherapy is widely employed, its non-specific nature can induce adverse effects on normal cells, prompting the exploration of targeted therapies. The 1,2,4-triazole scaffold has emerged as a promising element in anticancer drug development due to its structural diversity and potential to target cancer cells.
View Article and Find Full Text PDFAAPS PharmSciTech
January 2025
Department of Pharmaceutics, Manipal College of Pharmaceutical Sciences, Manipal Academy of Higher Education, Manipal, Karnataka, 576107, India.
The current study aims to establish a novel ultra-deformable vesicular system to enhance the drug penetration across the skin by preparing the ketoconazole-loaded menthosomes. It was achieved through regular thin-film evaporation & hydration techniques. To examine the effect of formulation parameters on menthosome characteristics, a 2 full factorial design was used using Design-Expert® software.
View Article and Find Full Text PDFBrain Behav
January 2025
Neuroscience Research Center, Institute of Neuropharmacology, Kerman University of Medical Sciences, Kerman, Iran.
Purpose: Essential tremor (ET) is a prevalent movement disorder, yet current therapeutic options remain limited. Emerging evidence implicates leucine-rich repeat and immunoglobulin-like domain-containing protein (Lingo-1) and neuroinflammation in the pathophysiology of ET. This study aimed to investigate whether agmatine, a biogenic amine neuromodulator attenuates tremors and modulates the expression of Lingo-1 and proinflammatory markers in a rodent model of ET.
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