ABSTRACT
A set of arylpiperazine derivatives with imide fragments, 1-(1H-pyrrol-1-ylmethyl)-10-oxa-4-azatricyclo[5.2.1.0(2,6)-]dec-8-ene-3,5-dione connected by propyl and butyl linkers, were synthesized and tested for the potential anxiolytic and antidepressant activities. Compounds 3a and 3b demonstrated antidepressant activity in the forced swimming tests in mice and were devoid of neurotoxic effects. (chimney test in mice).
Subject(s)
Anti-Anxiety Agents/chemical synthesis , Antidepressive Agents/chemical synthesis , Piperazines/chemical synthesis , Animals , Anti-Anxiety Agents/chemistry , Anti-Anxiety Agents/pharmacology , Antidepressive Agents/chemistry , Antidepressive Agents/pharmacology , Male , Mice , Motor Activity/drug effects , Piperazines/chemistry , Piperazines/pharmacologyABSTRACT
N-Substituted amides of endo-3-(3-methylthio-1,2,4-triazol-5-yl)bicyclo[2.2.1]hept-5-ene-2-carboxylic acid and 1-(5-methylthio-1,2,4-triazol-3-yl)cyclohexane-2-carboxylic acid were prepared by the condensation reaction of endo-S-methyl-N1-(bicyclo[2.2.1]hept-5-ene-2,3-dicarbonyl)isothiosemicarbazide and S-methyl-N1-(cyclohexane-2,3-dicarbonyl)isothiosemicarbazide with primary amines. The synthesized compounds were screened for their microbiological and pharmacological activities.
Subject(s)
Amides/chemistry , Analgesics/pharmacology , Carboxylic Acids/pharmacology , Analgesics/chemistry , Anti-Infective Agents/chemistry , Anti-Infective Agents/pharmacology , Bacteria/classification , Bacteria/drug effects , Carboxylic Acids/chemistry , Fungi/classification , Fungi/drug effects , Microbial Sensitivity TestsABSTRACT
3-[(1-Methylpyrrol-2-yl)methyl]-4-substituted 4,5-dihydro-1H-1,2,4-triazol-5-ones were obtained by the cyclization reaction of 1-[(1-methylpyrrol-2-yl)acetyl]-4-substituted semicarbazides in alkaline medium. The effects of the synthesized compounds of the central nervous system of mice were studied.
Subject(s)
Triazoles/pharmacology , Analgesics/pharmacology , Animals , Central Nervous System/drug effects , Drug Evaluation, Preclinical , Immobilization , Male , Mice , Psychomotor Performance/drug effects , Sleep/drug effects , Thiopental/pharmacology , Triazoles/chemistryABSTRACT
In the reaction of (2,4-dioxothiazolidin-5-yl)acetyl chloride with 1,2,4-triazole, 4-phenyl-1,2,4-triazolin-5-one and 4-phenyl-1,2,4-triazolin-5-thione, the new corresponding amides (2-4) were obtained. For compounds 2 and 4 effects on central nervous system (CNS) of mice were studied.
Subject(s)
Amides/chemical synthesis , Central Nervous System Agents/chemical synthesis , Thiazolidines/chemistry , Triazoles/chemistry , Amides/chemistry , Amides/pharmacology , Animals , Central Nervous System Agents/chemistry , Central Nervous System Agents/pharmacology , Male , MiceABSTRACT
New 3-(3,4-diaryl-1,2,4-triazole-5-yl)propenoic acid derivatives (8-14) were synthesized by condensation of N(3)-substituted amidrazones (1-7) with maleic anhydride. Molecular structure of obtained compounds was confirmed by an elemental analysis, IR and (1)H NMR spectra, and the X-ray crystallography for compound 11. The influence of the compound 9 on the central nervous system (CNS) of mice in some behavioural test was examined. The investigated compound showed anticonvulsive activity and potent antinociceptive action.
Subject(s)
Anticonvulsants/chemical synthesis , Pain Measurement/drug effects , Triazoles/chemical synthesis , Alkenes/chemical synthesis , Alkenes/pharmacology , Animals , Anticonvulsants/pharmacology , Male , Mice , Triazoles/pharmacologyABSTRACT
Synthesis of 3-(piperidin-4-yl)-4-substituted-D-2-1,2,4-triazoline-5-thione derivatives, AS-1-AS-4 is described. Results of a preliminary pharmacological screening of two compounds AS-1 and AS-3 are presented.
Subject(s)
Central Nervous System Agents/chemical synthesis , Central Nervous System Agents/pharmacology , Piperidines/chemical synthesis , Piperidines/pharmacology , Thiazoles/chemical synthesis , Thiazoles/pharmacology , 5-Hydroxytryptophan/pharmacology , Analgesics/chemical synthesis , Analgesics/pharmacology , Animals , Anti-Anxiety Agents/chemical synthesis , Anti-Anxiety Agents/pharmacology , Anticonvulsants/chemical synthesis , Anticonvulsants/pharmacology , Body Temperature/drug effects , Indicators and Reagents , Male , Mice , Pain Measurement , Psychomotor Performance/drug effects , Sleep/drug effectsABSTRACT
New derivatives of 1,2,4-triazoline-5-thione system were obtained. The effects of both these compounds AP-I (3-phenoxymethyl-4-phenyl-D2-1,2,4-triazoline-5-thione) and AP-II (3-phenoxymethyl-4-ethyl-D2-1,2,4-triazoline-5-thione) on the central nervous system (CNS) of mice were studied.
Subject(s)
Central Nervous System Agents/chemical synthesis , Central Nervous System Agents/pharmacology , Thiones/chemical synthesis , Thiones/pharmacology , Triazoles/chemical synthesis , Triazoles/pharmacology , 5-Hydroxytryptophan/pharmacology , Analgesics/chemical synthesis , Analgesics/pharmacology , Animals , Anti-Anxiety Agents/chemical synthesis , Anti-Anxiety Agents/pharmacology , Anticonvulsants/chemical synthesis , Anticonvulsants/pharmacology , Body Temperature/drug effects , Central Nervous System Agents/toxicity , Indicators and Reagents , Male , Mice , Pain Measurement , Psychomotor Performance/drug effects , Sleep/drug effectsABSTRACT
Eleven new derivatives of chelidonine I, obtained by functionalization of the alkaloid hydroxyl group, have been tested for CNS activity in mice exhibiting statistically significant effects.
Subject(s)
Alkaloids/chemistry , Alkaloids/pharmacology , Berberine Alkaloids , Central Nervous System/drug effects , Phenanthridines , Animals , Benzophenanthridines , Central Nervous System/physiology , Drug Evaluation, Preclinical/methods , Male , MiceABSTRACT
In the reaction of (4-phenyl- or 3,4-diphenyl-5-oxo-1,2,4-triazeolin-1-ylmethyl)-carbohydrazide (IIa, IIb) with isothiocyanates the thiosemicarbazide derivatives [IIIa, b - IXa, b] were obtained. Cyclization of those compounds in the presence of 2% or 10% NaOH led to formation of derivatives with the 1,2,4-triazolin-5-thione system [Xa, b - XV[a, b]. Molecular structure proposed for this group of compounds was confirmed by X-ray structure analysis of Xa and XIVa. Compounds Xa, XIIa and XIVa were investigated pharmacologically for their central properties in mice. It was shown that only compound XIIa produced antinociceptive effects in mice.
Subject(s)
Thiones/chemical synthesis , Thiones/pharmacology , Triazoles/chemical synthesis , Triazoles/pharmacology , Animals , Mice , Motor Activity/drug effects , Technology, Pharmaceutical/methods , Technology, Pharmaceutical/statistics & numerical data , Thiones/chemistry , Triazoles/chemistryABSTRACT
Synthesis of sulfur derivatives of indane-1,3-dione, VIIb-c, VIIIa-b, IX and X is described. Results of a preliminary pharmacological screening of six compounds [VIIb, VIII, VIIIb, IX, X and XI] are presented.
