Structure-activity correlations for the central nervous system depressant 2-imidazolidinones

1970 ◽  
Vol 13 (4) ◽  
pp. 623-626 ◽  
Author(s):  
Eric J. Lien ◽  
Mehdi. Hussain ◽  
Michael P. Golden
2019 ◽  
Vol 4 (1) ◽  
pp. 1
Author(s):  
Dini Kesuma

Synthesis of the 4-chlorobenzoylthiourea compound was carried out by acylating thiourea with 4-chlorobenzoyl chloride. The 4-chlorobenzoylthiourea compound  will increase the lipophilic and the electronic properties other than the lead compounds of benzoylthiourea in order to, by expectation, raise the central nervous system depressant as well. The lipophilic would affect the ability of the compounds in penetrating biological membranes, which is highly dependent on the solubility of the drug within lipid/water. Log P is the most common method used in determining the parameter value. This experiment was to mix two dissolvents (octanol and water) which are immissible. The both levels of the compounds were carefully observed by a spectrophotometer UV-Vis. From the test, the result of log P value of the 4-chlorobenzoylthiourea compound was 2.32, while the theoretical log P value of the compounds, by using the π Hansch-Fujita method is 1.62 and the f Rekker-Mannhold method is 2.225. Consequently, the result of the test shows that there is a significant difference between the progress experiment and both theoretical log P methods. Moreover, in the test of the central nervous system depressant through the potentiation test to thiopental using mice indicates that the 4-chlorobenzoylthiourea compound have potentiation effects to thiopental compared to the lead compounds of benzoylthiourea.


2012 ◽  
Vol 2 (1) ◽  
pp. 8
Author(s):  
Anindya Bose ◽  
Anuradha Khuntia ◽  
Jayanta Kumar Gupta ◽  
Sudam Si

The central nervous system (CNS) depressant activity of the ethanol extract (200 and 400 mg/kg) and its fractions (200 mg/kg each) of the aerial parts of Cleome rutidosperma was investigated in various models. The tested extract and its fractions showed significant (P<0.01) anxiolytic, anticonvulsant activity (in treating petit mal epilepsy) without any unwanted sedation effect. These findings justify the traditional use of this plant in CNS disorders.


2008 ◽  
Vol 8 (4) ◽  
pp. 448-451 ◽  
Author(s):  
Tasmina Rahman ◽  
Khandaker Ashfaqur Rahman ◽  
Sultana Rajia ◽  
Mahiuddin Alamgir ◽  
Mahmud Tareq Hassan Khan ◽  
...  

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