Abstract
In this study, the synthesis of a new series of 3,6-disubstituted-7H-1,2,4-triazolo[3,4-b][1,3,4]thiadiazine 1a-4c compounds derived from 4-amino-3-substituted-1,2,4-triazole-5-thiones 1-4 is described. All of the synthesized compounds were screened for their possible analgesic / anti-inflammatory, antioxidant activities and gastric toxicity. The compound 2c was found to have both significant analgesic and consistent anti-inflammatory activity without inducing any gastric lesions along with minimal lipid peroxidation. A deep insight into the structures of the active compounds revealed that the compounds carrying an electron withdrawing group (a chloride or fluoride) on the phenyl ring at 6-position of the condensed heterocyclic derivatives exhibited noticeable higher activity.
MeSH terms
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Acetic Acid
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Analgesics / chemical synthesis
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Analgesics / pharmacology*
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Animals
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Anti-Inflammatory Agents, Non-Steroidal / chemical synthesis
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Anti-Inflammatory Agents, Non-Steroidal / pharmacology*
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Antioxidants / chemical synthesis
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Antioxidants / pharmacology*
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Carrageenan
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Drug Evaluation, Preclinical
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Edema / chemically induced
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Edema / prevention & control
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Female
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Lipid Peroxidation
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Magnetic Resonance Spectroscopy
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Male
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Mice
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Mice, Inbred BALB C
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Spectrophotometry, Infrared
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Stomach Ulcer / chemically induced
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Stomach Ulcer / prevention & control
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Structure-Activity Relationship
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Thiadiazines / chemical synthesis
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Thiadiazines / pharmacology*
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Triazoles / chemical synthesis
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Triazoles / pharmacology*
Substances
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Analgesics
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Anti-Inflammatory Agents, Non-Steroidal
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Antioxidants
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Thiadiazines
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Triazoles
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Carrageenan
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Acetic Acid