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.
TY - JOUR
AU - Trišović, Nemanja
AU - Timić, Tamara
AU - Divljaković, Jovana
AU - Rogan, Jelena
AU - Poleti, Dejan
AU - Savić, Miroslav
AU - Ušćumlić, Gordana
PY - 2012
UR - http://TechnoRep.tmf.bg.ac.rs/handle/123456789/2189
AB - 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.
PB - Springer Wien, Wien
T2 - Monatshefte Fur Chemie
T1 - Synthesis, structural and biological characterization of 5-phenylhydantoin derivatives as potential anticonvulsant agents
EP - 1457
IS - 10
SP - 1451
VL - 143
DO - 10.1007/s00706-012-0791-8
ER -
@article{
author = "Trišović, Nemanja and Timić, Tamara and Divljaković, Jovana and Rogan, Jelena and Poleti, Dejan and Savić, Miroslav and Ušćumlić, Gordana",
year = "2012",
abstract = "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.",
publisher = "Springer Wien, Wien",
journal = "Monatshefte Fur Chemie",
title = "Synthesis, structural and biological characterization of 5-phenylhydantoin derivatives as potential anticonvulsant agents",
pages = "1457-1451",
number = "10",
volume = "143",
doi = "10.1007/s00706-012-0791-8"
}
Trišović, N., Timić, T., Divljaković, J., Rogan, J., Poleti, D., Savić, M.,& Ušćumlić, G.. (2012). Synthesis, structural and biological characterization of 5-phenylhydantoin derivatives as potential anticonvulsant agents. in Monatshefte Fur Chemie
Springer Wien, Wien., 143(10), 1451-1457.
https://doi.org/10.1007/s00706-012-0791-8
Trišović N, Timić T, Divljaković J, Rogan J, Poleti D, Savić M, Ušćumlić G. Synthesis, structural and biological characterization of 5-phenylhydantoin derivatives as potential anticonvulsant agents. in Monatshefte Fur Chemie. 2012;143(10):1451-1457.
doi:10.1007/s00706-012-0791-8 .
Trišović, Nemanja, Timić, Tamara, Divljaković, Jovana, Rogan, Jelena, Poleti, Dejan, Savić, Miroslav, Ušćumlić, Gordana, "Synthesis, structural and biological characterization of 5-phenylhydantoin derivatives as potential anticonvulsant agents" in Monatshefte Fur Chemie, 143, no. 10 (2012):1451-1457,
https://doi.org/10.1007/s00706-012-0791-8 . .
