Search Results - "Slavikova, Barbora"
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C‑3 Steroidal Hemiesters as Inhibitors of 17β-Hydroxysteroid Dehydrogenase Type 10
Published in ACS omega (12-03-2024)“…17β-HSD10 is a mitochondrial enzyme that catalyzes the steroidal oxidation of a hydroxy group to a keto group and, thus, is involved in maintaining steroid…”
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Correction to “C‑3 Steroidal Hemiesters as Inhibitors of 17β-Hydroxysteroid Dehydrogenase Type 10”
Published in ACS omega (09-04-2024)“…[This corrects the article DOI: 10.1021/acsomega.3c10148.]…”
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Access of inhibitory neurosteroids to the NMDA receptor
Published in British journal of pharmacology (01-06-2012)“…BACKGROUND AND PURPOSE NMDA receptors are glutamatergic ionotropic receptors involved in excitatory neurotransmission, synaptic plasticity and excitotoxic cell…”
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Strong Inhibitory Effect, Low Cytotoxicity and High Plasma Stability of Steroidal Inhibitors of N -Methyl-D-Aspartate Receptors With C-3 Amide Structural Motif
Published in Frontiers in pharmacology (12-11-2018)“…Herein, we report the synthesis, structure-activity relationship study, and biological evaluation of neurosteroid inhibitors of -methyl-D-aspartate receptors…”
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Chiral ligand induced geometrical type of isomerism in Schiff-base Copper(II) complexes with urease inhibitory activities
Published in Inorganica Chimica Acta (01-12-2023)“…[Display omitted] •Novel copper(II) complexes with Schiff-base ligands derived from 2-formylphenoxyacetic acid (fphaa) and DL-α-alanine, β-alanine, taurine,…”
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Docosahexaenoic Acid-Derived Fatty Acid Esters of Hydroxy Fatty Acids (FAHFAs) With Anti-inflammatory Properties
Published in Diabetes (New York, N.Y.) (01-09-2016)“…White adipose tissue (WAT) is a complex organ with both metabolic and endocrine functions. Dysregulation of all of these functions of WAT, together with…”
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Synthesis of Fluorinated Brassinosteroids Based on Alkene Cross-Metathesis and Preliminary Biological Assessment
Published in Journal of medicinal chemistry (24-09-2009)“…Three types of brassinosteroid analogues with perfluoroalkylated side chains were synthesized by using alkene cross-metathesis of a brassinosteroid derivative…”
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Allopregnanolone and Pregnanolone Analogues Modified in the C Ring: Synthesis and Activity
Published in Journal of medicinal chemistry (28-03-2013)“…(25R)-3β-Hydroxy-5α-spirostan-12-one (hecogenin) and 11α-hydroxypregn-4-ene-3,20-dione (11α-hydroxyprogesterone) were used as starting materials for the…”
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Synthetic testosterone derivatives modulate rat P2X2 and P2X4 receptor channel gating
Published in Journal of neurochemistry (01-07-2019)“…P2X receptors (P2XRs) are ATP‐gated cationic channels that are allosterically modulated by numerous compounds, including steroids and neurosteroids. These…”
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Positive Modulators of the N‑Methyl‑d‑aspartate Receptor: Structure–Activity Relationship Study of Steroidal 3‑Hemiesters
Published in Journal of medicinal chemistry (24-05-2018)“…Here, we report the synthesis of pregn-5-ene and androst-5-ene dicarboxylic acid esters and explore the structure–activity relationship (SAR) for their…”
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Lithocholic acid inhibits P2X2 and potentiates P2X4 receptor channel gating
Published in The Journal of steroid biochemistry and molecular biology (01-09-2020)“…•We tested a hypothesis that bile acids modulate activity of the rat P2X receptors.•We designed and synthesized several derivatives of lithocholic…”
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5β-reduced neuroactive steroids as modulators of growth and viability of postnatal neurons and glia
Published in The Journal of steroid biochemistry and molecular biology (01-05-2024)“…Endogenous neurosteroids (NS) and their synthetic analogs, neuroactive steroids (NAS), are potentially useful drug-like compounds affecting the pathophysiology…”
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A New Class of Potent N‑Methyl‑d‑Aspartate Receptor Inhibitors: Sulfated Neuroactive Steroids with Lipophilic D‑Ring Modifications
Published in Journal of medicinal chemistry (13-08-2015)“…N-Methyl-d-aspartate receptors (NMDARs) are glutamate-gated ion channels that play a crucial role in excitatory synaptic transmission. However, the…”
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Pregn-5-en-3β-ol and androst-5-en-3β-ol dicarboxylic acid esters as potential therapeutics for NMDA hypofunction: In vitro safety assessment and plasma stability
Published in Steroids (01-07-2019)“…[Display omitted] •In vitro safety evaluation of positive modulators of NMDA receptor.•NMDA receptor positive allosteric modulation as a potential therapeutic…”
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Screening of novel 3α5β-neurosteroids for neuroprotective activity against glutamate- or NMDA-induced excitotoxicity
Published in The Journal of steroid biochemistry and molecular biology (01-05-2019)“…[Display omitted] •3α5β-Neurosteroids suppress both glutamate- and NMDA-induced excitotoxicity.•Ca2+ entry and consequent ROS release and caspase-3 activation…”
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Neurosteroid-like Inhibitors of N‑Methyl‑d‑aspartate Receptor: Substituted 2‑Sulfates and 2‑Hemisuccinates of Perhydrophenanthrene
Published in Journal of medicinal chemistry (26-05-2016)“…N-Methyl-d-aspartate receptors (NMDARs) display a critical role in various diseases of the central nervous system. The activity of NMDARs can be modulated by…”
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Physicochemical and biological properties of novel amide-based steroidal inhibitors of NMDA receptors
Published in Steroids (01-01-2017)“…[Display omitted] •Synthesis of new amide-based inhibitors of NMDA receptors.•Strong inhibitors of NMDA currents.•The Caco-2 assay was used to evaluate…”
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Allopregnanolone (3α-Hydroxy-5α-pregnan-20-one) Derivatives with a Polar Chain in Position 16α: Synthesis and Activity
Published in Journal of medicinal chemistry (09-04-2009)“…The lipophilic nature of allopregnanolone prevents its user-friendly application in human medicine. On inspiration by previously prepared allopregnanolone with…”
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Brassinosteroids: Synthesis and Activity of Some Fluoro Analogues
Published in Journal of medicinal chemistry (10-07-2008)“…Three types of 5α-androstane and ergostane analogues of brassinolide, containing a fluorine atom in either the 3α or the 5α positions or in 3α and 5α…”
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