Anticonvulsant evaluation and docking analysis of VV‐Hemorphin‐5 analogues
Sign Up to like & getrecommendations! Published in 2019 at "Drug Development Research"
DOI: 10.1002/ddr.21514
Abstract: VV‐Hemorphin‐5 is an endogenous opioid peptide of the Hemorphin family with affinity at opioid receptors. A series of C‐amide analogues have been synthesized, based on the structure of VV‐Hemorphin‐5, modified at position 1 and 7… read more here.
Keywords: anticonvulsant activity; peptide; evaluation; test ... See more keywords
Comparative anticonvulsant activity of the GABAkine KRM‐II‐81 and a deuterated analog
Sign Up to like & getrecommendations! Published in 2023 at "Drug Development Research"
DOI: 10.1002/ddr.22042
Abstract: A series of imidazodiazepines has been developed that possess reduced sedative liabilities but retain efficacy in anticonvulsant screening models. The latest of these compounds, (5‐(8‐ethynyl‐6‐(pyridin‐2‐yl)‐4H‐benzo[f]imidazole[1,5‐α][1,4]diazepin‐3‐yl) oxazole known as KRM‐II‐81) is currently awaiting advancement into the… read more here.
Keywords: comparative anticonvulsant; krm; anticonvulsant activity; anticonvulsant ... See more keywords
Synthesis, anticonvulsant activity, and molecular modeling studies of novel 1-phenyl/1-(4-chlorophenyl)-2-(1H-triazol-1-yl)ethanol ester derivatives
Sign Up to like & getrecommendations! Published in 2018 at "Medicinal Chemistry Research"
DOI: 10.1007/s00044-018-2225-6
Abstract: A series of new ester derivatives were synthesized by the reaction of various acids with 1-phenyl/1-(4-chlorophenyl)-2-(1H-triazol-1-yl)ethanol and in vivo screened for their anticonvulsant activity. The title compounds were screened against MES and ScM seizure tests… read more here.
Keywords: anticonvulsant activity; ester derivatives; phenyl chlorophenyl; triazol ethanol ... See more keywords
Anticonvulsant Activity of Dimephosphonum
Sign Up to like & getrecommendations! Published in 2019 at "BioNanoScience"
DOI: 10.1007/s12668-019-0609-9
Abstract: A novel Russian medicine dimephosphonum at its therapeutic doses of 50 mg/kg and 100 mg/kg showed anti-seizure activity on models of primary generalized seizures caused by corazolum or by maximal electroshock in rats and mice. Dimephosphonum prevented… read more here.
Keywords: medicine; activity; anticonvulsant activity; dimephosphonum ... See more keywords
Design, synthesis and anticonvulsant activity of new imidazolidindione and imidazole derivatives.
Sign Up to like & getrecommendations! Published in 2020 at "Bioorganic chemistry"
DOI: 10.1016/j.bioorg.2020.104020
Abstract: New imidazolidindiones and tetra-substituted imidazole derivatives were designed, synthesized, and evaluated for the anticonvulsant activity through pentylenetetrazole (PTZ)-induced seizures and maximal electroshock (MES) tests using valproate sodium and phenytoin sodium as reference drugs, respectively. Most… read more here.
Keywords: design synthesis; anticonvulsant activity; imidazole derivatives; synthesis anticonvulsant ... See more keywords
Discovery of [1,2,4]-triazolo [1,5-a]pyrimidine-7(4H)-one derivatives as positive modulators of GABAA1 receptor with potent anticonvulsant activity and low toxicity.
Sign Up to like & getrecommendations! Published in 2019 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2019.111824
Abstract: In searching for more effective and safer antiepileptic drugs, a series of 2,5-disubstituted [1,2,4]-triazolo[1,5-a]pyrimidine-7(4H)-one derivatives were designed and synthesized. Spontaneous Ca2+ oscillations (SCOs) of cortical neurons were used for in vitro phenotypic screening. Maximal electroshock test… read more here.
Keywords: triazolo pyrimidine; anticonvulsant activity; pyrimidine one; one derivatives ... See more keywords
Molecular docking study and anticonvulsant activity of synthesized 4-((4,6-dimethyl-6H-1,3-thiazin-2-yl)phenylsulfonyl)urea/thiourea derivatives
Sign Up to like & getrecommendations! Published in 2017 at "Journal of King Saud University - Science"
DOI: 10.1016/j.jksus.2016.12.006
Abstract: Abstract A new series of 1-(4-substitutedphenyl)-3-(4-(4,6-dimethyl-6H-1,3-thiazin-2-yl)phenylsulfon-yl)urea/thiourea (3a–l) derivatives were synthesized and screened for anticonvulsant activity by maximal electro shock (MES) and pentylenetetrazole (PTZ) induced convulsant model. All the derivatives were evaluated for neurotoxicity measures by… read more here.
Keywords: thiourea derivatives; anticonvulsant activity; urea thiourea; dimethyl thiazin ... See more keywords
Identification of GSK-3 as a Potential Therapeutic Entry Point for Epilepsy.
Sign Up to like & getrecommendations! Published in 2019 at "ACS chemical neuroscience"
DOI: 10.1021/acschemneuro.8b00281
Abstract: In view of the clinical need for new antiseizure drugs (ASDs) with novel modes of action, we used a zebrafish seizure model to screen the anticonvulsant activity of medicinal plants used by traditional healers in… read more here.
Keywords: epilepsy; gsk potential; anticonvulsant activity; therapeutic entry ... See more keywords
Crystallographic studies of cinnamamide derivatives as a means of searching for anticonvulsant activity.
Sign Up to like & getrecommendations! Published in 2017 at "Acta crystallographica. Section C, Structural chemistry"
DOI: 10.1107/s2053229617013845
Abstract: A cinnamamide (3-phenylprop-2-enamide) core is present in many pharmacologically active compounds. We report three new crystal structures of N-substituted cinnamamide derivatives which were screened for anticonvulsant activity, namely (R,S)-(2E)-N-(2-hydroxypropyl)-3-phenylprop-2-enamide, C12H15NO2, (1), (R,S)-(2E)-N-(1-hydroxybutan-2-yl)-3-phenylprop-2-enamide, C13H17NO2, (2), and… read more here.
Keywords: anticonvulsant activity; cinnamamide derivatives; phenylprop enamide; studies cinnamamide ... See more keywords
Anticonvulsant Activity of trans-Anethole in Mice
Sign Up to like & getrecommendations! Published in 2022 at "BioMed Research International"
DOI: 10.1155/2022/9902905
Abstract: Epilepsy is a chronic neurological disorder affecting 1-2% of world population, and one-third of patients are refractory to pharmacological treatment. This fact has stimulated research for new antiepileptic drugs and natural products have been an… read more here.
Keywords: seizure; anticonvulsant activity; eeg profile; anethole mice ... See more keywords
Synthesis and Anticonvulsant Activity of α-Amino Acid Amide Derivatives
Sign Up to like & getrecommendations! Published in 2019 at "Current Bioactive Compounds"
DOI: 10.2174/1573407214666180530081328
Abstract: Epilepsy is a disease of the central nervous system that affects approximately 50 million individuals worldwide. Although several new drugs have been marketed in the last 25 years, almost one-third of patients are not protected.… read more here.
Keywords: seizure; anticonvulsant activity; activity; amino acid ... See more keywords