Central nervous system active compounds. VI. Reissert compounds as precursors of 1-(3-phthalidy1)isoquinolines

1981 ◽  
Vol 34 (1) ◽  
pp. 151 ◽  
Author(s):  
TV Hung ◽  
BA Mooney ◽  
RH Prager ◽  
AD Ward
Keyword(s):  
Central Nervous System ◽  
Nervous System ◽  
Phase Transfer ◽  
Active Compounds ◽  
Central Nervous System Depressant ◽  
Reissert Compounds

The reactions of isoquinoline and phthalazine Reissert compounds with phthalaldehydic acids and their derivatives have been investigated as a means of synthesizing 1-(3-phthalidyl)isoquinolines. Of a variety of conditions tried those involving phase transfer were found, in general, to be the most suitable. The products, which are analogues of the convulsant alkaloid bicuculline, showed weak central nervous system depressant activity.

PENENTUAN NILAI PARAMETER LIPOFILITAS SENYAWA 4-KLOROBENZOILTIOUREA DAN UJI POTENSIASI TERHADAP TIOPENTAL PADA MENCIT PUTIH (Mus musculus)

2019 ◽  
Vol 4 (1) ◽  
pp. 1
Author(s):  
Dini Kesuma
Keyword(s):  
Central Nervous System ◽  
Nervous System ◽  
Electronic Properties ◽  
Mus Musculus ◽  
Log P ◽  
P Value ◽  
Lead Compounds ◽  
Significant Difference ◽  
Central Nervous System Depressant ◽  
The Central Nervous System

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.

5-(2-Aminoethyl)-2-oxazolidinones with central nervous system depressant and antiinflammatory activity

1973 ◽  
Vol 16 (10) ◽  
pp. 1129-1132 ◽  
Author(s):  
William J. Welstead ◽  
Grover C. Helsley ◽  
C. Roy Taylor ◽  
Lennox B. Turnbull ◽  
John P. Da Vanzo ◽  
...  
Keyword(s):  
Central Nervous System ◽  
Nervous System ◽  
Antiinflammatory Activity ◽  
Central Nervous System Depressant

scholarly journals Lavandulae aetheroleum Oil: A Review on Phytochemical Screening, Medicinal Applications, and Pharmacological Effects

2020 ◽  
Vol 11 (3) ◽  
pp. 9836-9847
Keyword(s):  
Central Nervous System ◽  
Clinical Pharmacology ◽  
Nervous System ◽  
Chemical Constituents ◽  
Cardiovascular Effects ◽  
Pharmacological Effects ◽  
Lavandula Angustifolia ◽  
Experimental Pharmacology ◽  
Central Nervous System Depressant ◽  
Anti Inflammatory

Lavandulae aetheroleum, the oil, was obtained by vapor condensation from the flower of Lavandula angustifolia Mill. or Lavandula intermedia Loisel (Lamiaceae) plant. Other names of Lavandulae aetheroleum oil are Al birri, common or English lavender. The Lavandula angustifolia Mill. or Lavandula intermedia Loisel plant is spreading in the Mediterranean, southern Europe, Bulgaria, Russia, and USA. The Lavandula angustifolia Mill. or Lavandula intermedia Loisel plant, is an odor shrub with 1-2 m in height. The oil is a clear, colorless, or pale yellow. The gas chromatography studies reported the following percentage of the major chemical constituents in the oil: linalyl acetate (25-46%), linalool (20-45%), terpinen-4-ol (1.2-6.0%), lavendulyl acetate (> 1.0%), 1,8-cineole (1,8-cineol, cineol, cineole, eucalyptol) (< 2.5%), 3-octanone (< 2.5%), camphor (< 1.2%), limonene (< 1.0%), and α-terpineol (< 2.0%). Medicinal applications of the oil include the treatment of restlessness, anxiety, cardiovascular disorders, insomnia, and gastrointestinal disorders, burns, diarrhea, headache, sore throats, and wounds. Pharmacological effects include experimental and clinical pharmacology. Experimental pharmacology includes anesthetic, anticonvulsant, sedative, anti-inflammatory, antimicrobial, antispasmodic, antispasmodic, central nervous system depressant effects. Clinical pharmacology includes anxiolytic, analgesic, and cardiovascular effects. The oil dose by inhalation = 0.06-0.2 ml/ 3 times/day while oil dose internally = 1-4 drops approximately 20-80 mg on a sugar cube per day. In conclusion, Lavandulae aetheroleum oil had an anesthetic, anticonvulsant, sedative, anti-inflammatory, antimicrobial, antispasmodic, antispasmodic, central nervous system depressant, anxiolytic, analgesic, and cardiovascular effects.

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