3784-93-8Relevant academic research and scientific papers
Synthesis, structural and biological characterization of 5-phenylhydantoin derivatives as potential anticonvulsant agents
Trisovic, Nemanja,Rogan, Jelena,Poleti, Dejan,Uscumlic, Gordana,Timic, Tamara,Divljakovic, Jovana,Savic, Miroslav M.
, p. 1451 - 1457,7 (2020/08/20)
Considering the importance of hydantoin derivatives in treatment of status epilepticus, four 5-phenylhydantoins, whose lipophilicities were estimated to be similar to that of phenytoin, were synthesized. Evaluation of their anticonvulsant activities was performed on rats by subcutaneous pentylenetetrazol seizure test and intravenous pentylenetetrazol threshold test, and spontaneous locomotor activity test was used to assess possible sedative effects. X-ray analysis of three compounds suggested that certain analogies might be drawn between interactions in crystal packing and biological interactions responsible for their anticonvulsant activity. It was found that 5-ethyl-5-phenyl- 3-propylhydantoin exhibits the most favorable pharmacological properties among the synthesized compounds, i.e., anticonvulsant activity comparable to phenytoin with lower liability for induction of sedation in rats.
Synthesis, structure, and solvatochromic properties of pharmacologically active 5-substituted 5-phenylhydantoins
Trisovic, Nemanja,Valentic, Natasa,Erovic, Marko,Dakovic-Sekulic, Tatjana,Uscumlic, Gordana,Juranic, Ivan
experimental part, p. 1227 - 1234 (2012/06/04)
A series of 5-substituted 5-phenylhydantoins was synthesized and their UV absorption spectra were recorded in the region 200-400 nm in selected solvents of different polarity. The effects of solvent dipolarity/polarizability and solvent-solute hydrogen-bonding interactions were analyzed by means of the linear solvation energy relationship concept proposed by Kamlet and Taft. The lipophilicities of the investigated hydantoins were estimated by calculation of their log P values. The quantitative relationship between the ratio of the contributions of specific solvent interactions and the corresponding lipophilicity parameter is discussed. The correlation equations were combined with the corresponding ED50 values and different physicochemical parameters to generate new equations that demonstrate the reasonable relationships between solute-solvent interactions and the structure-activity parameters. In order to determine a spectroscopic assignment of the absorption bands in different solvents, quantum chemical calculations were done. Springer-Verlag 2011.
NOVEL 2-AMINO-IMIDAZOLE-4-ONE COMPOUNDS AND THEIR USE IN THE MANUFACTURE OF A MEDICAMENT TO BE USED IN THE TREATMENT OF COGNITIVE IMPAIRMENT, ALZHEIMER’S DISEASE, NEURODEGENERATION AND DEMENTIA
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Page/Page column 77, (2008/06/13)
This invention relates to novel compounds having the structural formula I below and to their pharmaceutically acceptable salts, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cognitive impairment, Alzheimer Di
