Synthesis and anticonvulsant activity of some N-(benzoyl)glycinanilide derivatives


SOYER Z., AKGÜL Ö., TARİKOĞULLARI DOĞAN A. H. , Calis U.

MEDICINAL CHEMISTRY RESEARCH, cilt.22, ss.4708-4714, 2013 (SCI İndekslerine Giren Dergi) identifier identifier

  • Cilt numarası: 22 Konu: 10
  • Basım Tarihi: 2013
  • Doi Numarası: 10.1007/s00044-013-0474-y
  • Dergi Adı: MEDICINAL CHEMISTRY RESEARCH
  • Sayfa Sayıları: ss.4708-4714

Özet

Glycine is a major inhibitory neurotransmitter and recent studies have shown that certain lipophilic glycine derivatives demonstrate anticonvulsant activity in animal epilepsy models. On the other hand, anilide is another fruitful structure for designing potential anticonvulsant agents. Ameltolide, ralitoline and some phthalimide derivatives are the examples of anilide analogs with potent anticonvulsant activity. In this study, two key structural pharmacophores were combined and a series of N-benzoylglycinanilide derivatives were designed. Their anticonvulsant activities evaluated against maximal electroshock (MES) and subcutaneous metrazole seizure tests, whereas their neurotoxicity was examined by rotarod test. The preliminary screening results indicated that majority of the compounds were effective in the MES test. None of the compounds showed neurotoxicity according to the rotarod test at studied doses. The most active compound in the series is N-(2-((4-methoxyphenyl)amino)-2-oxoethyl)benzamide (compound 8) which bearing 4-methoxy substituent on the N-phenyl ring.