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A new series of d-glucose-conjugated 2,3-thiazoline-benzo-[]-thiazole hybrid compounds - were synthesized from reaction of the corresponding thioureas - and ethyl bromoacetate in the presence of sodium acetate in chloroform. The evaluations for anti-Alzheimer activity showed that some compounds exhibited remarkable inhibitory activity against AChE and BChE as well as against MAO-A and MAO-B enzymes. The orders of inhibition for each enzyme of these compounds were as follows: > (against AChE), > (against BChE), > > (against MAO-A), and > (against MAO-B). Compound was an inhibitor of interest due to its potent or good activity against the two studied enzymes BChE and MAO-B, respectively. Compounds (against AChE) and (against (BChE) had a competitive type with constants of 16.93 and 17.09 nM, respectively. The most potential compounds , , and were not cytotoxic on 3T3 cells and had high levels of safety.
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http://dx.doi.org/10.1021/acsmedchemlett.5c00064 | DOI Listing |
Chem Biodivers
September 2025
Department of Biology, Faculty of Science, Selçuk University, Konya, Turkey.
Hippophae salicifolia, commonly known as sea buckthorn, is native to the Indian Himalayan region. This study is the first to comprehensively assess the phytochemical profile and biological activities of H. salicifolia leaves extracted through maceration, infusion, and percolation (Soxhlet apparatus) methods.
View Article and Find Full Text PDFACS Omega
September 2025
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Anadolu University, 26470 Eskişehir, Turkey.
Ten novel pyrazoline-thiazole derivatives were synthesized and assessed for their potential as acetylcholinesterase and butyrylcholinesterase inhibitors. The structure of the target compounds was characterized by H NMR and C NMR, and purity was determined using HPLC. The in vitro enzyme inhibitory activity assays determined that compounds (IC = 0.
View Article and Find Full Text PDFBioorg Chem
August 2025
Department of Chemistry, Faculty of Science, Atatürk University, 25240 Erzurum, Türkiye. Electronic address:
Compounds that possess a benzene sulfonamide structure are utilized in a wide range of fields. Benzene bissulfonamides are also important compounds in the field of organic and medicinal chemistry. Based on these features, a series of benzene bissulfonamides were synthesized in moderate yields starting from 3-methylanisole.
View Article and Find Full Text PDFFood Sci Nutr
September 2025
Physiology and Biochemistry Laboratory, Department of Biology, Science Faculty Selcuk University Konya Turkey.
The current investigation was designed to explore the chemical composition, antioxidant capacity, enzyme inhibitory activity, and cytotoxic potential of four different extracts (Ethyl Acetate, Ethanol, Ethanol/Water (70%) and Water) derived from the aerial parts of . In vitro, assessments were performed utilizing diverse antioxidant assays, along with evaluations of neuroprotective enzyme inhibition targeting acetylcholine and butyl choline enzymes, as well as antidiabetic activities against α-amylase and α-glucosidase and a potential candidate for a tyrosinase inhibitor. LC-ESI-QTOF-MS identification provided a total of 70 compounds in the extracted samples of , including kaempferol 3-(deoxyhexosyl-hexoside)-7-hexoside, rutin, quercetin dideoxyhexoside, caffeic acid hexoside, quinoline alkaloids, morphine derivatives, and scoulerine.
View Article and Find Full Text PDFFront Toxicol
August 2025
Programa de Epidemiología, Escuela de Salud Pública, Facultad de Medicina, Universidad de Chile, Santiago, Chile.
Background: Unintentional pesticide poisoning is a global health concern, disproportionately affecting agricultural workers in developing countries due to inadequate regulations and limited access to protective equipment. While questionnaires offer a cost-effective alternative for assessing organophosphate (OP) pesticide exposure compared to urinary (e.g.
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