Synthesis, structural and biological characterization of 5-phenylhydantoin derivatives as potential anticonvulsant agents
Samo za registrovane korisnike
2012
Autori
Trišović, NemanjaTimić, Tamara
Divljaković, Jovana
Rogan, Jelena
Poleti, Dejan
Savić, Miroslav
Ušćumlić, Gordana
Članak u časopisu (Objavljena verzija)
Metapodaci
Prikaz svih podataka o dokumentuApstrakt
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.
Ključne reči:
Hydantoin derivatives / Anticonvulsant activity / Sedative effects / Crystal structureIzvor:
Monatshefte Fur Chemie, 2012, 143, 10, 1451-1457Izdavač:
- Springer Wien, Wien
Finansiranje / projekti:
- Proučavanje sinteze, strukture i aktivnosti organskih jedinjenja prirodnog i sintetskog porekla (RS-MESTD-Basic Research (BR or ON)-172013)
DOI: 10.1007/s00706-012-0791-8
ISSN: 0026-9247
WoS: 000309253500015
Scopus: 2-s2.0-84867096117
Institucija/grupa
Tehnološko-metalurški fakultetTY - 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 . .