ABSTRACT
A series of 1,2,4-triazolyl-thiophene and 1,2,4-triazolyl-pyrazole carboxylic acid derivatives was tested for acute toxicity and nonsteroidal anti-inflammatory activity. Some of these compounds showed potent analgesic activity and interesting nonsteroidal anti-inflammatory properties in different acute and chronic inflammation models.
Subject(s)
Anti-Inflammatory Agents, Non-Steroidal/pharmacology , Carboxylic Acids/pharmacology , Triazoles/pharmacology , Analgesics, Non-Narcotic/pharmacology , Animals , Arthritis, Experimental/drug therapy , Arthritis, Experimental/pathology , Bleeding Time , Carboxylic Acids/toxicity , Carrageenan , Ear, External/pathology , Edema/chemically induced , Edema/pathology , Edema/prevention & control , Gossypium , Granuloma/drug therapy , Granuloma/pathology , Male , Mice , Pain Measurement/drug effects , Rats , Rats, Wistar , Stomach Ulcer/chemically induced , Triazoles/toxicityABSTRACT
A series of 1,2,4-triazolyl heterocarboxylic derivatives were tested for acute toxicity and CNS effects in mice. Several of these compounds demonstrated clear psychostimulant effects. Other components of the series, however, showed a definite central depressant activity. Some of the screened derivatives showed interesting anxiolytic properties.
Subject(s)
Central Nervous System Agents/chemical synthesis , Heterocyclic Compounds, 2-Ring/chemical synthesis , Triazoles/chemical synthesis , Animals , Anti-Anxiety Agents/chemical synthesis , Anti-Anxiety Agents/pharmacology , Anti-Anxiety Agents/toxicity , Apomorphine/toxicity , Behavior, Animal/drug effects , Central Nervous System Agents/pharmacology , Central Nervous System Agents/toxicity , Dopamine Agonists/toxicity , Drug Synergism , Female , Heterocyclic Compounds, 2-Ring/pharmacology , Heterocyclic Compounds, 2-Ring/toxicity , Hypnotics and Sedatives/pharmacology , Male , Mice , Motor Activity/drug effects , Muscarinic Agonists/toxicity , Muscle Relaxants, Central/chemical synthesis , Muscle Relaxants, Central/pharmacology , Muscle Relaxants, Central/toxicity , Oxotremorine/toxicity , Pentobarbital/pharmacology , Sleep/drug effects , Triazoles/pharmacology , Triazoles/toxicityABSTRACT
A series of 4-phenyl-2-thioxo-benzo[4,5]thieno[2,3-d]pyrimidine derivatives endowed with anti-inflammatory and related pharmacological properties were submitted to a more extensive study to know their exact pharmacological profile and their possible side effects. The studied compounds possess a remarkable analgesic activity, devoid of central effects. They also show an interesting anti-inflammatory profile evidenced by their effectiveness in different experimental models of inflammation. In addition, these compounds exhibit none or very little activity on CNS, scarce toxicity and low gastrointestinal aggressivity.
Subject(s)
Anti-Inflammatory Agents, Non-Steroidal/chemical synthesis , Pyrimidines/chemical synthesis , Animals , Anti-Inflammatory Agents, Non-Steroidal/pharmacology , Anti-Inflammatory Agents, Non-Steroidal/toxicity , Bleeding Time , Female , Male , Mice , Pyrimidines/pharmacology , Pyrimidines/toxicity , Rats , Rats, Wistar , Stomach Ulcer/chemically induced , Stomach Ulcer/pathologyABSTRACT
As an extension of a previous work, in which a number of 4H-pyrrolo-[1,2-a]thieno[2,3-f][1,4]diazepines were described, a new series of derivatives of the isomeric pyrrolo[1,2-a]thieno[3,2-f]diazepines ring system has been synthesized. The products obtained, together with those reported in the previous paper, were tested for acute toxicity and CNS activity in mice.
Subject(s)
Anti-Anxiety Agents/chemical synthesis , Azepines/chemical synthesis , Pyrroles/chemical synthesis , Animals , Anti-Anxiety Agents/pharmacology , Anti-Anxiety Agents/toxicity , Azepines/pharmacology , Azepines/toxicity , Behavior, Animal/drug effects , Body Temperature/drug effects , Female , Male , Mice , Pyrroles/pharmacology , Pyrroles/toxicityABSTRACT
A new series of 11-substituted 6,11-dihydro-6-methyl-dibenzo[c,f]-[1,2]thiazepine S,S-dioxides was synthesized. Some of the components show significant anticonvulsant activity in the MES, pentetrazol and strychnine tests. The more active compounds are devoid of neurotoxic effects.
