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1,3,4-Oxadiazole Sulfonamide Derivatives Containing Pyrazole Structures: Design, Synthesis, Biological Activity Studies, and Mechanism Study.
J Agric Food Chem
January 2025
National Key Laboratory of Green Pesticide, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Center for R&D of Fine Chemicals of Guizhou University, Guiyang 550025, China.
Sulfonamide derivatives have been widely used for pesticide research in recent years. Herein, 1,3,4-oxadiazole sulfonamide derivatives containing a pyrazole structure were synthesized, and their structure-activity relationship was studied. Bioactivity tests showed the remarkable efficacy of most synthesized compounds.
View Article and Find Full Text PDFImportance of Modulating Kynurenic Acid Metabolism-Approaches for the Treatment of Dementia.
Biomolecules
January 2025
Karl Landsteiner Research Institute for Neurochemistry, Neuropharmacology, Neurorehabilitation and Pain Therapy, 3362 Mauer-Amstetten, Austria.
In this article, we focus on kynurenic acid metabolism in neuropsychiatric disorders and the biochemical processes involved in memory and cognitive impairment, followed by different approaches in the fight against dementia. Kynurenic acid-a biochemical part of L-tryptophan catabolism-is synthesized from L-kynurenine by kynurenine aminotransferases. Experimental pharmacological studies have shown that elevated levels of kynurenic acid in the brain are associated with impaired learning and that lowering kynurenic acid levels can improve these symptoms.
View Article and Find Full Text PDFTryptophan-specific modification and diversification of peptides and proteins.
Org Biomol Chem
January 2025
Department of Chemistry, Muragachha Government College, Nadia 741154, West Bengal, India.
In spite of being the second-lowest abundant proteinogenic amino acid, approximately 90% of proteins contain at least one tryptophan residue. Hence, the chemoselective functionalization of tryptophan residue can provide access to site-selective bioconjugation of almost all known proteins. With the increase in the utility of bioconjugated proteins and peptides as drugs and therapeutic agents, the development of smart protocols to fabricate and modulate biomolecules has flourished.
View Article and Find Full Text PDF[Adiposity-related anthropometric parameters, indoles and atherosclerotic cardiovascular disease in Chinese adults: a prospective cohort study].
Zhonghua Liu Xing Bing Xue Za Zhi
January 2025
Department of Epidemiology and Biostatistics, School of Public Health, Peking University, Beijing100191, China Peking University Center for Public Health and Epidemic Preparedness & Response, Beijing100191, China Key Laboratory of Epidemiology of Major Diseases (Peking University), Ministry of Education, Beijing100191, China State Key Laboratory of Vascular Homeostasis and Remodeling, Peking University, Beijing100191, China.
To investigate the relationship of several adiposity-related anthropometric parameters, including BMI, waist circumference (WC), waist-to-hip ratio (WHR), body fat percentage (BFP) and indoles in plasma with the incidence of atherosclerotic cardiovascular disease (ASCVD) in adults in China. In China Kadoorie Biobank (CKB) study, blood samples were collected from 2 183 participants in the first resurvey in 2008 to detect indoles. Participants' body weight, body height, WC, hip circumference, and BFP were measured at baseline survey in 2004 and resurvey in 2008, the BMI and WHR were calculated with standardized methods.
View Article and Find Full Text PDFTransformation-Guided Genome Mining Provides Access to Brominated Lanthipeptides.
Org Lett
January 2025
School of Chemistry and Biochemistry, Georgia Institute of Technology, Atlanta, Georgia 30332, United States.
Natural product biosynthesis is nature's tinkering ground for developing new enzymes that can achieve chemical transformations that are outside the purview of traditional chemical catalysis. Herein we describe a genome mining approach that leads to the discovery of a halogenase that regioselectively brominates a tryptophan side chain indole for a macrocyclic peptide substrate, enabling downstream chemical arylation by Suzuki-Miyaura coupling. The halogenase was found to prefer a macrocyclic peptide substrate over a linear peptide.
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