ABSTRACT
New N-(5-methylisoxazol-3-yl)-2 or 3 or 4-(phenoxyacetamido)benzamides 6a-t were synthesized and tested for their in vitro antimicrobial activity against gram positive (Staphylococcus aureus ATCC 25923) and gram negative (Escherichia coli ATCC 25922 and Pseudomonas aeruginosa ATCC 27853) bacteria as well as fungi (Candida albicans ATCC 10231, Candida tropicalis ATCC 13803 and Cryptococcus neoformans ATCC 90112). Compounds 6 were devoid of antibacterial as well as antifungal activities at maximum tested concentrations of 50 micrograms/ml for bacteria and 100 micrograms/ml for yeast.
Subject(s)
Acetamides/chemical synthesis , Anti-Infective Agents/chemical synthesis , Anti-Infective Agents/pharmacology , Bacteria/drug effects , Fungi/drug effects , Phenyl Ethers/chemical synthesis , Acetamides/pharmacology , Anti-Bacterial Agents , Gram-Negative Bacteria/drug effects , Gram-Positive Bacteria/drug effects , Indicators and Reagents , Magnetic Resonance Spectroscopy , Microbial Sensitivity Tests , Phenyl Ethers/pharmacologyABSTRACT
Several new 1-methyl-5-[substituted-4-oxo-1,2,3-benzotriazin-3-yl] -1H-pyrazole-4-acetic acids and their ethyl ester derivatives were prepared. The compounds were tested for analgesic and antiinflammatory activities, acute toxicity, ulcerogenic effect, and as in vitro inhibitors of 3 alpha-hydroxysteroid dehydrogenase (3 alpha-HSD), since it is claimed that the inhibition of such an enzyme predicts in vivo antiinflammatory activity. Some compounds were more active than phenylbutazone in the phenylbenzoquinone and acetic acid peritonitis tests, and equiactive to the same drug in the carrageenin paw edema test. All the compounds inhibited the 3 alpha-HSD, but no correlation was observed with the paw edema inhibition values. The compounds proved to possess marginal or no ulcerogenic effect, as well as low systemic toxicity.
Subject(s)
3-Hydroxysteroid Dehydrogenases/antagonists & inhibitors , Analgesics/chemical synthesis , Anti-Inflammatory Agents/chemical synthesis , Enzyme Inhibitors/chemical synthesis , Pyrazoles/chemical synthesis , 3-alpha-Hydroxysteroid Dehydrogenase (B-Specific) , Analgesics/pharmacology , Animals , Anti-Inflammatory Agents/pharmacology , Enzyme Inhibitors/pharmacology , Male , Mice , Pyrazoles/pharmacology , RatsSubject(s)
3-Hydroxysteroid Dehydrogenases/antagonists & inhibitors , Enzyme Inhibitors/chemical synthesis , Pyrazoles/chemical synthesis , Pyrimidinones/chemical synthesis , Enzyme Inhibitors/pharmacology , Magnetic Resonance Spectroscopy , Pyrazoles/pharmacology , Pyrimidinones/pharmacology , Spectrophotometry, InfraredABSTRACT
The synthesis of some pyrazolo [4,3-e] [1,4] diazepin-5,8-diones has been accomplished starting from the readily available 1-ethyl-3-methyl-4-nitro-5-pyrazolecarbonylchloride and the appropriate alpha-aminoesthers, 2a, b, c. The catalytic reduction of the obtained 3a, b, c gave the products 4a, b, c which were, in turn, cyclized into the title compounds 5a, b, c. The intermediates of type 3 and 4 and the pyrazolo-diazepin-diones 5 were tested in vitro for their antimicrobial activity.
Subject(s)
Anti-Bacterial Agents/chemical synthesis , Azepines/chemical synthesis , Bacteria/drug effects , Anti-Bacterial Agents/pharmacology , Azepines/pharmacology , Microbial Sensitivity TestsSubject(s)
Azepines/chemical synthesis , Central Nervous System Agents/chemical synthesis , Pyrazoles/chemical synthesis , Animals , Azepines/pharmacology , Behavior, Animal/drug effects , Central Nervous System Agents/pharmacology , Conflict, Psychological , Discrimination, Psychological/drug effects , Drinking Behavior/drug effects , Male , Motor Activity/drug effects , Pentobarbital/pharmacology , Pentylenetetrazole/pharmacology , Pyrazoles/pharmacology , Rats , Rats, Inbred Strains , Time Perception/drug effectsABSTRACT
New imidazolylpyrazoles were synthesized and tested for antimicrobial activities. The compounds did not show any significant activity.
Subject(s)
Anti-Infective Agents/chemical synthesis , Imidazoles/chemical synthesis , Pyrazoles/chemical synthesis , Anti-Bacterial Agents , Bacteria/drug effects , Fungi/drug effects , Imidazoles/pharmacology , Microbial Sensitivity Tests , Pyrazoles/pharmacologyABSTRACT
The synthesis of 1-phenyl-5,8-dimethyl-1,4,5,6,7,8-hexahydro-pyrazolo[3,4-e][1,4] diazepin-4,7-dione and of 1-phenyl-3,5,8-trimethyl-1,4,5,6,7,8-hexahydro-pyrazolo[3,4-e] [1,4]diazepin-4,7-dione is described. These compounds exhibit activity on CNS in animals.
