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 - Trisović, Nemanja
AU - Timić, Tamara
AU - Divljaković, Jovana
AU - Rogan, Jelena
AU - Poleti, Dejan
AU - Savić, Miroslav
AU - Uscumlić, Gordana
PY - 2012
UR - https://farfar.pharmacy.bg.ac.rs/handle/123456789/1649
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 für Chemie Chemical Monthly
T1 - Synthesis, structural and biological characterization of 5-phenylhydantoin derivatives as potential anticonvulsant agents
VL - 143
IS - 10
SP - 1451
EP - 1457
DO - 10.1007/s00706-012-0791-8
ER -
@article{
author = "Trisović, Nemanja and Timić, Tamara and Divljaković, Jovana and Rogan, Jelena and Poleti, Dejan and Savić, Miroslav and Uscumlić, 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 für Chemie Chemical Monthly",
title = "Synthesis, structural and biological characterization of 5-phenylhydantoin derivatives as potential anticonvulsant agents",
volume = "143",
number = "10",
pages = "1451-1457",
doi = "10.1007/s00706-012-0791-8"
}
Trisović, N., Timić, T., Divljaković, J., Rogan, J., Poleti, D., Savić, M.,& Uscumlić, G.. (2012). Synthesis, structural and biological characterization of 5-phenylhydantoin derivatives as potential anticonvulsant agents. in Monatshefte für Chemie Chemical Monthly
Springer Wien, Wien., 143(10), 1451-1457.
https://doi.org/10.1007/s00706-012-0791-8
Trisović N, Timić T, Divljaković J, Rogan J, Poleti D, Savić M, Uscumlić G. Synthesis, structural and biological characterization of 5-phenylhydantoin derivatives as potential anticonvulsant agents. in Monatshefte für Chemie Chemical Monthly. 2012;143(10):1451-1457.
doi:10.1007/s00706-012-0791-8 .
Trisović, Nemanja, Timić, Tamara, Divljaković, Jovana, Rogan, Jelena, Poleti, Dejan, Savić, Miroslav, Uscumlić, Gordana, "Synthesis, structural and biological characterization of 5-phenylhydantoin derivatives as potential anticonvulsant agents" in Monatshefte für Chemie Chemical Monthly, 143, no. 10 (2012):1451-1457,
https://doi.org/10.1007/s00706-012-0791-8 . .
