YURISTA AVIANTI HANUM, 050610028 (2012) PENGARUH GUGUS TRIFLUOROMETIL PADA CINCIN BENZENA TERHADAP AKTIVITAS PENEKAN SISTEM SARAF PUSAT SENYAWA 3-TRIFLUOROMETIL BENZOILUREA. Skripsi thesis, UNIVERSITAS AIRLANGGA.

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Abstract

Benzoylurea had non cyclic ureides structure like barbitutare derivatives as central nervous system (CNS) depressants. Some benzoylurea derivatives had been synthesized and tested for the CNS depressant activity. It had been studied that their CNS depressant activity were influenced by lipofilicity. In this research, 3- trifluoromethyl benzoylurea which is the derivatives of benzoylurea, was tested as CNS depressant, to investigate the effect of trifluoromethyl substituent on the benzene ring of benzoylurea structure on CNS depressant activity of 3-trifluoromethyl benzoylurea. Based on π value trifluoromethyl substituent has higher lipophilicity that could increase the lipophilicity of benzoylurea. In spite of the lipophilicity, 3-trifluoromethyl benzoylurea had σ and MR value higher than benzoylurea. It could be expected that 3- trifluoromethyl benzoylurea has CNS depressant activity higher than benzoylurea. CNS depressant activity was tested by Barbituric Sleeping Time method using thiopental Na as sleep inducer. The 3- trifluoromethyl benzoylurea in the dose of 25, 50 and 100 mg/kg body-weight were given as suspension in CMC Na 0.5% via intraperitonial injection. After 60 minutes, thiopental solution was injected in the dose of 60 mg/kg body-weight. The CNS depressant activity was expressed as increasing precentage of sleeping time. The result showed that 3-trifluoromethyl benzoylurea in dose of 50 and 100 mg/kg body-weight could prolonged the sleeping time of thiopental which indicate that 3-trifluoromethyl benzoylurea had CNS depressant activity. Compare with benzoylurea, 3- trifluoromethyl benzoylurea had higher activity. It could be concluded that the CNS depressant activity of 3-trifluoromethyl benzoylurea was higher than benzoylurea

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