The current article discusses the activities of several synthesized metal heterochelates in in-vitro as anti-ulcer agents followed by their docking study. For this purpose, two important ligands like 8-hydroxyquinoline and DL-methionine were used in synthesis of heterochelates of metal including Cr (III), Mn (II), Fe (III), Co (II), Ni (II), Cu (II), Zn (II), Cd (II) and Pb (II). It was observed that these complexes showed excellent urease inhibition activities in which thiourea was the standard having IC value 21.6 ± 0.12μM. The Cu (II) complex showed potent inhibitory activity (22.6 ± 0.72 μM) when compared with the standard thiourea (21.6±0.12μM) among the nine synthesized complexes while Mn (II), Fe (III), Cd (II) and Pb (II) also showed better inhibitory activities. The urease inhibitory activities of hetercochelates also tested and validated by docking analysis.
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ChemMedChem
December 2024
University of Ljubljana, Faculty of Pharmacy, Askerceva cesta 7, 1000, Ljubljana, SLOVENIA.
Seven different enzymes comprise the galactosyltransferases family, of which β-1,4-galactosyltransferase I (β-1,4-GALT1) is the major contributor to galactosylation activity in cells. Since abnormalities in galactosylation are associated with many pathophysiological conditions, β-1,4-GALT1 is an interesting new target for drug discovery and molecular probe design. There are several known β-1,4-GALT1 inhibitors, but most of them suffer from low cell permeability and thus low in vivo activity.
View Article and Find Full Text PDFPhys Rev Lett
December 2024
Laboratoire de Physique Théorique et Modélisation, CY Cergy Paris Université, CNRS, UMR 8089, 95302 Cergy-Pontoise cedex, France.
Despite the fact that neural dynamics is triggered by discrete synaptic events, the neural response is usually obtained within the diffusion approximation representing the synaptic inputs as Gaussian noise. We derive a mean-field formalism encompassing synaptic shot noise for sparse balanced neural networks. For low (high) excitatory drive (inhibitory feedback) global oscillations emerge via continuous or hysteretic transitions, correctly predicted by our approach, but not from the diffusion approximation.
View Article and Find Full Text PDFChem Biodivers
December 2024
M'sila University, Department of Natural and Life Sciences, Road Bordj Bou Arreiridj, M'sila 28000 Algeria, M'sila, ALGERIA.
The study examines the chemical composition and antimicrobial properties of petroleum ether and hydro-methanolic extracts of Achillea santolina(A. santolina) from Algeria. Chemical profiling was performed using High-Performance Liquid Chromatography with Diode Array Detection (HPLC-DAD) for the hydro-methanolic extract and Gas Chromatography-Mass Spectrometry (GC-MS) for the petroleum ether extract.
View Article and Find Full Text PDFChem Biodivers
December 2024
Shandong University, Marine college, Wenhuaxi road 180, 264209, Weihai, CHINA.
The present study investigated the chemical composition of essential oil from Tetrapanax papyrifer and evaluated its antioxidant and anti-α-glucosidase activity. Sixty-one essential oil compounds from Tetrapanax papyrifer were identified by gas chromatography-mass spectrometry (GC-MS) and gas chromatography-flame ionization detector (GC-FID). The essential oil is rich in sesquiterpenoids (96.
View Article and Find Full Text PDFChem Biodivers
December 2024
Daffodil International University, Pharmacy, Dhaka 1207, 1207, Dhaka, BANGLADESH.
The study investigates the inhibitory properties of Mangiferin and Friedelin against glucokinase, DPP-IV, α-amylase, and α-glucosidase using computational methods, in vitro enzyme assays, and in-depth ADMET analysis. The study utilized a computer-aided drug design approach to assess the potential therapeutic properties of Mangiferin and Friedelin as T2DM therapeutic agents. Molecular docking studies' outcomes encouraged the evaluation of both compounds in in vitro enzymatic assays.
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