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Molecules, Vol. 26, Pages 6124: A Novel Phenylpyrrolidine Derivative: Synthesis and Effect on Cognitive Functions in Rats with Experimental Ishemic Stroke
Vladimir P. Chekhonin Sophia S. Borisevich Maxim A. Gureev Anastasia D. Shagina Nina M. Kiseleva Vadim V. Negrebetsky Yuri I. Baukov We performed an in silico, in vitro, and in vivo assessment of a potassium 2-[2-(2-oxo-4-phenylpyrrolidin-1-yl) acetamido]ethanesulfonate (compound 1) as a potential prodrug for cognitive function improvement in ischemic brain injury. Using in silico methods, we predicted the pharmacological efficacy and possible safety in rat models. In addition, in silico data showed neuroprotective features of compound 1, which were further supported by in vitro experiments in a glutamate e...
Source: Molecules - October 11, 2021 Category: Chemistry Authors: Denis A. Borozdenko Aiarpi A. Ezdoglian Tatiana A. Shmigol Darya I. Gonchar Dmitri N. Lyakhmun Dmitri V. Tarasenko Yaroslav V. Golubev Elvira A. Cherkashova Daria D. Namestnikova Ilya L. Gubskiy Alexey A. Lagunin Leonid V. Gubsky Vladimir P. Chekhonin Sop Tags: Article Source Type: research

Synthesis, Molecular Modeling of Novel Substituted Pyridazinones and Their Vasorelaxant activities.
Abstract BACKGROUND: Hypertension, one of the most common cardiovascular diseases that can cause coronary disease, stroke, myocardial infarction and sudden death, it is the major contributor to cardiac failure as well as renal insufficiency. OBJECTIVES: As there are many cardio-active pyridazinone-base derivatives in clinical use, therefore, it we aimed to synthesize a new series of pyridazin-3-ones and evaluate their vasorelaxant activity. METHODS: The new series of synthesized compounds were carried out first by synthesis of 6-flouroarylpyridazinones by cyclization of 3-(4-flourobenzoyl) propionic acid...
Source: Medicinal Chemistry - March 26, 2020 Category: Chemistry Authors: Ismail M, Soliman D, Elmoniem MHA, Jaleel GARA Tags: Med Chem Source Type: research

Astrocytic potassium and calcium channels as integrators of the inflammatory and ischemic CNS microenvironment
Biol Chem. 2021 Aug 30. doi: 10.1515/hsz-2021-0256. Online ahead of print.ABSTRACTAstrocytes are key regulators of their surroundings by receiving and integrating stimuli from their local microenvironment, thereby regulating glial and neuronal homeostasis. Cumulating evidence supports a plethora of heterogenic astrocyte subpopulations that differ morphologically and in their expression patterns of receptors, transporters and ion channels, as well as in their functional specialisation. Astrocytic heterogeneity is especially relevant under pathological conditions. In experimental autoimmune encephalomyelitis (EAE), a mouse m...
Source: Biological Chemistry - August 29, 2021 Category: Chemistry Authors: Samantha Schmaul Nicholas Hanuscheck Stefan Bittner Source Type: research

Highly efficient radiosynthesis and biological evaluation of 18Fsafinamide, a radiolabelled anti-parkinsonian drug for PET imaging
ChemMedChem. 2022 Sep 6. doi: 10.1002/cmdc.202200472. Online ahead of print.ABSTRACTAs an add-on drug approved for Parkinson's disease treatment, safinamide has multiple functions, such as selective and reversible monoamine oxidase-B inhibition, voltage-sensitive sodium/potassium channel blockage, and glutamate release inhibition. Meanwhile, safinamide shows tremendous therapeutic potential in the context of other central nervous system diseases (e.g., ischaemic stroke, amyotrophic lateral sclerosis, depression, etc.). In this work, [18F]safinamide, which is safinamide labelled by the positron-emitting radionuclide [18F]fl...
Source: ChemMedChem - September 7, 2022 Category: Chemistry Authors: Yangyang Xu Peili Cen Lijuan Ma Mei Tian Xue Zhang Qinghua Zhang Kaiwu Yu Hong Zhang Wangjun Gu Qinggang He Source Type: research

Discovery of a brain-sparing GIRK1/4 inhibitor for pharmacological cardioversion of atrial fibrillation
Bioorg Med Chem Lett. 2023 Mar 14:129237. doi: 10.1016/j.bmcl.2023.129237. Online ahead of print.ABSTRACTAtrial fibrillation (AF) is the most common cardiac arrhythmia, and a significant risk factor for ischemic stroke and heart failure. Marketed anti-arrhythmic drugs can restore sinus rhythm, but with limited efficacy and significant toxicities, including potential to induce ventricular arrhythmia. Atrial-selective ion channel drugs are expected to restore and maintain sinus rhythm without risk of ventricular arrhythmia. One such atrial-selective channel target is GIRK1/4 (G-protein regulated inwardly rectifying potassium...
Source: Bioorganic and Medicinal Chemistry Letters - March 16, 2023 Category: Chemistry Authors: Stefan Peukert Hatice Gulgeze Efthymiou Ruowei Mo Yunshan Peng Fupeng Ma Guillaume Barbe Gregory Bebernitz Cary Fridrich Chiara Buono Eric T Williams Thomas Daniels Lisha Li Xia Zhang Yuichiro Adachi Mie Abe Andrew K P Taggart Source Type: research