ABSTRACT
Newly synthesized indolylimidazolones were tested for their in vitro monoamine oxidase (MAO) inhibitory activity. These compounds were found to possess analgesic activity and anticonvulsant activity against maximal electroshock-induced convulsions in mice. The low toxicity of these compounds was reflected by their high approximate LD50 values.
Subject(s)
Analgesics , Anticonvulsants , Imidazoles/pharmacology , Monoamine Oxidase Inhibitors , Animals , In Vitro Techniques , Lethal Dose 50 , Mice , RatsABSTRACT
A new series of 2,3-cyclopentano-3,4-dihydro-4-spirocyclopentano-1,5-benzodi azepine which are substituted in 5-position with beta-N-heterocycloethyl or gamma-N-heterocyclo-n-propyl groups have been synthesized and evaluated for their CNS depressant activity including anticonvulsant, analgesic and pentobarbital induced hypnosis. These compounds were also investigated for their ability to inhibit in vitro succinate dehydrogenase (SDH). In most of the compounds an appreciable CNS depressant activity has been found to be associated with the compounds possessing good SDH inhibitory activity. Low toxicity of these compounds was reflected by their high approximate LD50 values.
Subject(s)
Anti-Anxiety Agents/chemical synthesis , Central Nervous System Depressants/chemical synthesis , Analgesics/chemical synthesis , Animals , Anti-Anxiety Agents/pharmacology , Anti-Anxiety Agents/toxicity , Anticonvulsants/chemical synthesis , Benzodiazepines , Central Nervous System Depressants/pharmacology , Central Nervous System Depressants/toxicity , Drug Synergism , Female , Lethal Dose 50 , Male , Mice , Pentobarbital/pharmacology , Sleep/drug effects , Succinate Dehydrogenase/antagonists & inhibitors , Time FactorsABSTRACT
Sixteen new 1,2-disubstituted-4-(indol-3'-yl)methylene imidazol-5-ones were synthesized by the condensation of oxazolone with different aryl amines and evaluated as to their anti-inflammatory and antiproteolytic activities. These derivatives showed 2-38% protection against carrageenin-induced paw oedema in albino rats at a dose of 100 mg/kg p.o. All compounds showed antiproteolytic activity. The degree of inhibition against trypsin-induced hydrolysis of casein ranged from 10 to 75% at a concentration of 4 X 10(-4) mol/l. Furthermore, active compounds of the series were also screened for their analgesic activity against aconitine-induced writhing in albino mice. The toxicity of the compounds was reflected by their approximate LD50 values.
Subject(s)
Anti-Inflammatory Agents, Non-Steroidal , Imidazoles/pharmacology , Indoles/pharmacology , Animals , Anti-Inflammatory Agents, Non-Steroidal/toxicity , Caseins , Edema/prevention & control , Female , Hydrolysis , Imidazoles/toxicity , Indoles/toxicity , Lethal Dose 50 , Male , Mice , Peptic Ulcer/chemically induced , Rats , Trypsin InhibitorsABSTRACT
Hematological changes and concurrent enzymatic activities in various tissues were determined in rats injected parentally with Iomex, a petroleum derivate and proposed weedicide. Among the hematological parameters studied only the differential leucocytic count showed significant alterations. This was indicated by a significant decrease in the number of lymphocytes and an increase in those of neutrophils. Significant differences were not observed in the levels of acid phosphatase, glutamic oxaloacetic, and glutamic pyruvate transaminase activities in brain and liver of the experimental group of animals.
