Abstract
Synthesis of 2-[2-hydroxy-3-(4-aryl-1-piperazinyl)propyl] derivatives of 4-alkoxy-6-methyl-1H-pyrrolo[3,4-c]pyridine-1,3(2H)-diones (8-12) is described. The chlorides used in the above synthesis can exist in two isomeric forms: chain (18-20) and cyclic (19a, 20a). The compounds 8-12 exhibited potent analgesic activity which was superior than that of acetylsalicylic acid in two different tests. Most of the investigated imides suppressed significantly spontaneous locomotor activity in mice.
MeSH terms
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Analgesics, Non-Narcotic / chemical synthesis*
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Analgesics, Non-Narcotic / pharmacology*
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Analgesics, Non-Narcotic / toxicity
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Animals
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Blood Pressure / drug effects
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Crystallography, X-Ray
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Dose-Response Relationship, Drug
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Female
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Indicators and Reagents
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Magnetic Resonance Spectroscopy
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Male
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Mice
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Models, Molecular
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Molecular Conformation
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Motor Activity / drug effects
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Pain Measurement / drug effects
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Piperazines / chemical synthesis*
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Piperazines / pharmacology*
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Pyridones / chemical synthesis*
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Pyridones / pharmacology*
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Pyrroles / chemical synthesis*
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Pyrroles / pharmacology*
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Rats
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Rats, Wistar
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Structure-Activity Relationship
Substances
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Analgesics, Non-Narcotic
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Indicators and Reagents
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Piperazines
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Pyridones
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Pyrroles