Abstract
This study is concerned with the synthesis of new 1,2,4-triazoles, 1,3,4-thiadiazoles, and 1,3,4-thiadiazines derivatives. Derivatives 3a-i were obtained by condensation of 4-amino-3-(4-pyridine)-5-mercapto-1,2,4-triazole 1 with the appropriate aldehyde. Compounds 4a-i were synthesized in a one pot reaction involving compounds 3a-i, formaldehyde, and morpholine. Condensation of compound 1 with the appropriate acids or 4-substituted phenacyl bromide gave compounds 6a-d and 8a-f respectively. The chemical structures of the newly synthesized derivatives were elucidated using different spectral and elemental methods of analysis. All compounds were evaluated for their anti-inflammatory activity and the most potent derivatives were tested for their analgesic activity using indomethacin as a reference drug. In addition, ulcerogenicity and LD(50) for the most active compounds were evaluated. Moreover, the antibacterial activities of the newly synthesized derivatives were investigated.
MeSH terms
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Analgesics* / chemical synthesis
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Analgesics* / pharmacology
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Analgesics* / toxicity
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Animals
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Anti-Bacterial Agents* / analysis
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Anti-Bacterial Agents* / chemical synthesis
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Anti-Bacterial Agents* / chemistry
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Anti-Bacterial Agents* / pharmacology
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Anti-Bacterial Agents* / toxicity
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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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Anti-Inflammatory Agents, Non-Steroidal* / toxicity
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Dose-Response Relationship, Drug
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Drug Evaluation, Preclinical
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Edema / chemically induced
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Edema / drug therapy
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Escherichia coli / drug effects
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Escherichia coli / growth & development
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Hot Temperature
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Lethal Dose 50
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Male
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Methicillin-Resistant Staphylococcus aureus / drug effects
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Methicillin-Resistant Staphylococcus aureus / growth & development
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Mice
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Microbial Sensitivity Tests
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Rats
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Stomach Ulcer / chemically induced
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Thiadiazoles* / chemical synthesis
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Thiadiazoles* / chemistry
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Thiadiazoles* / pharmacology
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Thiadiazoles* / toxicity
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Thiones* / chemical synthesis
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Thiones* / chemistry
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Thiones* / pharmacology
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Thiones* / toxicity
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Time Factors
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Triazoles* / chemical synthesis
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Triazoles* / chemistry
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Triazoles* / pharmacology
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Triazoles* / toxicity
Substances
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Analgesics
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Anti-Bacterial Agents
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Anti-Inflammatory Agents, Non-Steroidal
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Thiadiazoles
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Thiones
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Triazoles