ABSTRACT
Nineteen title compounds (1-3, Fig. 1) have been synthesised by Mannich reaction of the corresponding 2,6-disubstituted-quinazolones, 2-substituted-indole and formaldehyde. Some of them have been found to be CNS stimulants while some others were CNS depressants. Compounds 2c and 2d have been found to possess good anticonvulsant activity in MES protection test at the dose level of 100 mg/kg.
Subject(s)
Brain/drug effects , Quinazolines/chemical synthesis , Animals , Anticonvulsants/pharmacology , Central Nervous System Depressants/chemical synthesis , Central Nervous System Stimulants/chemical synthesis , Chemical Phenomena , Chemistry , Female , Male , Mice , Quinazolines/pharmacology , Reserpine/antagonists & inhibitors , Tremorine/antagonists & inhibitorsABSTRACT
5-Arylidene barbituric acids (1--5, Fig. 1) were obtained by the Perkin's condensation between the corresponding aryl aldehyde and active methylene group of barbituric acid. By the condensation of these 5-arylidene barbituric acids with different alkyl/aryl-chloroacids, fifteen new N,N'bis[potassium-alkyl/aryl carboxylate]-5-arylidene barbituric acids (6--8 Fig. 1) were prepared. Eight of the fifteen final compounds were screened for their pharmacological actions on CNS. They have shown irregular behavioral changes on the CNS; some of them were the CNS stimulants, whereas others were CNS depressants at 1/5 of ALD50 dose level (316--1000 g/kg).
Subject(s)
Barbiturates/chemical synthesis , Central Nervous System Agents/chemical synthesis , Central Nervous System Depressants/chemical synthesis , Animals , MiceABSTRACT
Twenty eight compounds have been synthesized in the series 2-substituted-3-[(N-alkanol-N-imidazolin-2'-ylamino)methyl]indoles. Some of them have been shown to protect mice from tremorine-induced tremors. The compounds are central nervous system depressants and relatively non-toxic.
Subject(s)
Indoles/pharmacology , Tremor/drug therapy , Animals , Central Nervous System/drug effects , Female , Indoles/chemical synthesis , Indoles/toxicity , Lethal Dose 50 , Male , MiceABSTRACT
Ten 1-(4-substituted-thiazol-2-yl)hydantoins have been synthesized. Some of them have shown antitubercular activity against Mycobacterium smegmatis.
Subject(s)
Hydantoins/pharmacology , Mycobacterium/drug effects , Hydantoins/chemical synthesisABSTRACT
Sixteen title compounds have been synthesized and some of them have shown interesting results in antiinflammatory screening against carrageenin-induced inflammation. In addition, the compounds were found to be central nervous system depressants and relatively non-toxic.
