Abstract
In this study, a new class of 4-amino-3-substituted-1,2,4-triazole-5-thiones (1-4) and their corresponding condensed derivatives 3,6-disubstituted 7H-1,2,4-triazolo[3,4-b]-1,3,4-thiadiazines (1a-4c) were synthesized and evaluated for their analgesic/anti-inflammatory activities. All synthesized compounds were also tested for their gastric toxicity and antioxidant activity on acute administration. Most of the compounds showed significant activity in both carrageenan-induced oedema and acetic acid-induced writhing tests besides negligible gastrointestinal toxicity. The compounds showing less ulcerogenic effect also showed less lipid peroxidation (LPO) level. Most promising results were obtained with the compounds that placed a fluoro or a chloride on the phenyl ring at the sixth position of the fused ring.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Analgesics / adverse effects
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Analgesics / chemical synthesis
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Analgesics / chemistry*
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Analgesics / therapeutic use*
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Animals
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Anti-Inflammatory Agents / adverse effects
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Anti-Inflammatory Agents / chemical synthesis
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Anti-Inflammatory Agents / chemistry*
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Anti-Inflammatory Agents / therapeutic use*
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Antioxidants / chemical synthesis
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Antioxidants / chemistry
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Antioxidants / therapeutic use
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Carrageenan
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Edema / chemically induced
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Edema / drug therapy
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Female
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Male
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Mice
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Mice, Inbred BALB C
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Models, Molecular
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Molecular Structure
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Pain Measurement / drug effects
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Thiadiazines / adverse effects
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Thiadiazines / chemical synthesis
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Thiadiazines / chemistry*
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Thiadiazines / therapeutic use*
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Triazoles / adverse effects
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Triazoles / chemical synthesis
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Triazoles / chemistry
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Triazoles / therapeutic use
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Ulcer / etiology
Substances
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Analgesics
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Anti-Inflammatory Agents
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Antioxidants
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Thiadiazines
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Triazoles
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1,2,4-triazole
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Carrageenan