Synthesis of some novel 1-(2-naphthyl)-2-(imidazol-1-yl)ethanone oxime ester derivatives and evaluation of their anticonvulsant activity

KARAKURT A., ALAGOZ M. A., Sayoglu B., Calis U., DALKARA S.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, cilt.57, ss.275-282, 2012 (SCI-Expanded) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 57
  • Basım Tarihi: 2012
  • Doi Numarası: 10.1016/j.ejmech.2012.08.037
  • Dergi Adı: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Sayfa Sayıları: ss.275-282
  • Anahtar Kelimeler: Oxime ester, (arylalkyl)imidazole, Azole derivatives, Anticonvulsant activity, E/Z isomers, ANTIMICROBIAL ACTIVITIES, ANTIEPILEPTIC DRUGS, ETHER DERIVATIVES, AGENTS, DENZIMOL, EPILEPSY
  • İnönü Üniversitesi Adresli: Evet

Özet

Twenty-three new oxime ester derivatives of nafimidone were synthesized with the prospect of potential anticonvulsant activities. MES and ScM tests were employed for their anticonvulsant activities and rotorod test for neurological deficits. Eighteen compounds were found to be protective against MES seizures. Alkyl (1-8) and arylalkyl (9,10) oxime ester derivatives were found to be more active than aryl oxime ester derivatives (11-23). Five compounds (2, 3, 7, 9, 10), which were protective at 0.5 h at the doses of 30 mg/kg and higher in MES test, showed the highest activity. Compound 17 was the most active one in ScM test at all dose levels at 4 h. (C) 2012 Elsevier Masson SAS. All rights reserved.