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Chemical Behavior and Bioactive Properties of Spinorphin Conjugated to 5,5'-Dimethyl- and 5,5'-Diphenylhydantoin Analogs.
Pharmaceuticals (Basel)
June 2024
Material Physics Laboratory, Physics Department, Universitas Negeri Makassar (UNM), Makassar 90223, Indonesia.
Article Synopsis
- The study focuses on synthesizing and characterizing new peptide derivatives derived from spinorphin, aiming to explore their potential as therapeutic agents, particularly in treating seizures and possibly other biological activities.
- Various characterization techniques, including scanning electron microscopy and spectroscopic methods, revealed structural changes in the peptides that correlate with their biological effects, particularly in combating seizures.
- The spinorphin derivatives showed notable anticonvulsant activity against multiple phases of seizures, with certain analogs demonstrating effectiveness against drug-resistant epilepsy, indicating their potential for broader therapeutic applications.
Comparative Analysis of Anticonvulsant Activity of and 5,5'-Diphenylhydantoin Schiff Bases.
Int J Mol Sci
November 2023
Department of Biology, Medical University of Pleven, 5800 Pleven, Bulgaria.
Recently, the four 5,5'-diphenylhydantoin Schiff bases, possessing different aromatic species () were synthesized, characterized, and evaluated for anticonvulsant activity in combination with phenytoin. In the present study, the and compounds were selected, based on their anticonvulsant potency, and compared with their isomers, prepared after a one-hour exposure to the UV source, for their anticonvulsant potency in the maximal electroshock (MES) test and the kainate (KA)-induced status epilepticus (SE) test in mice. In the MES test, the compound exhibited superior to phenytoin and isomer activity in the three tested doses, while the compound entirely suppressed the electroshock-induced seizure spread at the highest dose of 40 mg/kg.
View Article and Find Full Text PDFAdditive Anticonvulsant Profile and Molecular Docking Analysis of 5,5'-Diphenylhydantoin Schiff Bases and Phenytoin.
Biomedicines
October 2023
Institute of Biodiversity and Ecosystem Research, Bulgarian Academy of Sciences, 1113 Sofia, Bulgaria.
Four 5,5'-diphenylhydantoin Schiff bases possessing different aromatic species (-) were recently synthesized and characterized using spectroscopic and electrochemical tools. The present study aimed to ascertain the anticonvulsant activity of the novel phenytoin derivatives , , , and , containing different electron-donor and electron-acceptor groups, and their possible mechanism of action. The exhibited the highest potency to suppress the seizure spread with ED = 8.
View Article and Find Full Text PDFOccurrence and distribution of priority pharmaceuticals in the Yellow River and the Huai River in Henan, China.
Environ Sci Pollut Res Int
May 2020
Key Laboratory for Yellow River and Huai River Water Environment and Pollution Control, Ministry of Education, Henan Key Laboratory for Environmental Pollution Control, School of Environment, Henan Normal University, Xinxiang, 453007, Henan, People's Republic of China.
The occurrence and spatial distribution of priority pharmaceuticals (PPs) in water samples from the Yellow River and the Huai River in the Henan region of China were investigated in this study. The concentration of the total PPs (ΣPPs; sum of the 10 observed PPs) ranged from not detected to 3474 ng L in samples from the Yellow River and from 4.35 to 146 ng L in samples from the Huai River.
View Article and Find Full Text PDFSynthesis, anticancer, apoptosis-inducing activities and EGFR and VEGFR2 assay mechanistic studies of 5,5-diphenylimidazolidine-2,4-dione derivatives: Molecular docking studies.
Saudi Pharm J
July 2019
Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia.
A new series of 5,5-diphenylhydantoin derivatives containing benzylidene or isatin (-) was synthesized. Their anticancer activity against HeLa, a cervical cancer cell line, A549, a lung cancer cell line, and MDA-MB-231, a breast cancer cell line, was evaluated. Compounds , , and exhibited potent anticancer activity with average IC values against the tested cell lines of 109, 59, 81 and 113 μM, respectively.
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