Synthesis and anticonvulsant activity of substituted thiourea derivatives

Abstract

ABSTRACT: Twelve new thiourea derivatives were prepared by the reacting of 4-aminophenylacetic
acide with substituted isothiocyanates. Their chemical structures were proved by
means of IR, 1H-NMR, mass spectroscopic and elemental analyses. These compounds were
tested at dose of 50 mg/kg for their anticonvulsant activity using by pentylenetetrazole induced
seizure (PTZ) and maximal electroshock seizure (MES) tests in mice. Compound 1b,
(4-{[(4-chlorophenyl)thiocarbamoyl]amino}phenyl)acetic acid, was found to be more active
than the other tested compounds. The compound 1b reduced convulsions in all types of
grades (from grade I to V), therefore it increased convulsive threshold. It also increased
onset time from 1.20 to 2.58 sec. and survival % from 50 to 95.
KEY WORDS: Synthesis, thiourea, anticonvulsant activity.

Keywords

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Synthesis and anticonvulsant activity of substituted thiourea derivatives

Abstract

4-Aminofenilasetik asitin sübstitüe izotiyosiyanatlar ile reaksiyonu sonucu, on iki adet yeni tiyoüre bileşiği sentezlenmiştir. Bileşiklerin kimyasal yapıları IR, 1H-NMR, kütle spektroskopisi ve elementel analiz testleri ile aydınlatılmıştır. Tüm bileşiklerin antikonvulsan aktiviteleri 50mg/kg dozda farelerde pentilentetrazol (PTZ) ve maksimal elektroşok nöbet (MES) testleri kullanılarak tayin edilmiştir. Bileşik 1b’nin (4-{[(4-klorofenil)tiyokarbamoil]amino}fenil)asetik asit, diğer bileşiklere oranla daha aktif olduğu saptanmıştır. Tüm seviyelerde konvulsiyon oranını düşüren 1b bileşiği aynı zamanda nöbet eşiğini de yükseltmiştir. Ayrıca nöbet başlangıç süresini 1.20 saniyeden 2.58 saniyeye, hayatta kalma oranını ise %50’den %95’e yükseltmiştir

Keywords

• ANAHTAR KELİMELER: Sentez, tiyoüre, antikonvulsan aktivite

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