A convenient and efficient synthesis of novel achiral and chiral heterocyclic amino acid-like building blocks was developed. Regioisomeric methyl 5-(-Boc-cycloaminyl)-1,2-oxazole-4-carboxylates were prepared by the reaction of β-enamino ketoesters (including azetidine, pyrrolidine or piperidine enamines) with hydroxylamine hydrochloride. Unambiguous structural assignments were based on chiral HPLC analysis, H, C, and N NMR spectroscopy, HRMS, and single-crystal X-ray diffraction data.
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http://dx.doi.org/10.3762/bjoc.18.11 | DOI Listing |
Org Lett
January 2025
Advanced Research Institute and Department of Pharmaceutical Sciences, Taizhou University, Taizhou, Zhejiang 318000, People's Republic of China.
Herein, we present a metal-free, concise, and efficient protocol for the intermolecular reaction of amides (lactams) with donor-acceptor α-diazo esters to afford the functionalized α-amino-α-aroylethanoates. -Methyl-2-pyrrolidone (NMP) and ,-dimethylformamide (DMF) are employed as both reagents and solvents, allowing for the incorporation of all units into the products. The reaction is processed by the ester group migration and compatible with a broad range of substrates up to 50 examples.
View Article and Find Full Text PDFClin Neuropharmacol
January 2025
MedStar Georgetown University Hospital, Washington, DC.
Introduction: Adjunctive therapies to treat OFF episodes resulting from long-term levodopa treatment in Parkinson disease (PD) are hampered by safety and tolerability issues. Istradefylline offers an alternative mechanism (adenosine A2A receptor antagonist) and therefore potentially improved tolerability.
Methods: A systematic review of PD adjuncts published in 2011 was updated to include randomized controlled trials published from January 1, 2010-April 15, 2019.
Environ Toxicol Chem
January 2025
School of Environment and Energy, South China University of Technology, Guangzhou, PR China.
As a representative agent of bicyclic antidepressants, venlafaxine (VEN) has become widely used worldwide and is frequently detected in surface waters with concentrations ranging from ng/L to µg/L. To evaluate the toxicological effects of such medications on aquatic species, studies on environmentally relevant concentrations are essential. Zebrafish were used as a model organism to assess growth and development in larvae and examine tissue accumulation, oxidative stress, and DNA methylation in adults.
View Article and Find Full Text PDFEnviron Toxicol Chem
January 2025
Laboratorio de Desarrollo Analítico y Quimiometría (LADAQ), Cátedra de Química Analítica I, Facultad de Bioquímica y Ciencias Biológicas, Universidad Nacional del Litoral (UNL), Santa Fe, Argentina.
This study assesses the occurrence of emerging contaminants (ECs) from agricultural and livestock production activities along the Salado River (Santa Fe province, Argentina). Of the 23 ECs studied, 8 were detected and quantified in river and wastewater samples, including ciprofloxacin, enrofloxacin, chlorpyrifos-methyl, albendazole, fenbendazole, levamisole, diazepam, and thiamethoxam. In river samples, the highest concentrations corresponded to ciprofloxacin, chlorpyrifos-methyl, and enrofloxacin.
View Article and Find Full Text PDFProc Natl Acad Sci U S A
January 2025
Department of Anatomy, University of Otago, Dunedin 9016, New Zealand.
Aging is a complex process characterized by biological decline and a wide range of molecular alterations to cells, including changes to DNA methylation. In this study, we used a male-specific epigenetic marker of aging to build an epigenetic predictor that measures long-term androgen exposure in sheep and mice (median absolute error of 4.3 and 1.
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