Novel 3,6-Disubstituted 7H-1,2,4-Triazolo[3,4-b][1,3,4]thiadiazines: Synthesis, Characterization, and Evaluation of Analgesic / Anti-inflammatory, Antioxidant Activities
| Autor: | Birsen Tozkoparan, Göknur Aktay, Sevim Peri Aytaç |
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| Rok vydání: | 2009 |
| Předmět: |
Male
Magnetic Resonance Spectroscopy Antioxidant Spectrophotometry Infrared medicine.drug_class Stereochemistry medicine.medical_treatment Analgesic Drug Evaluation Preclinical Pharmaceutical Science Carrageenan Chloride Antioxidants Anti-inflammatory Lipid peroxidation Mice Structure-Activity Relationship Acetic acid chemistry.chemical_compound Drug Discovery medicine Animals Edema Structure–activity relationship Stomach Ulcer Acetic Acid Analgesics Mice Inbred BALB C Thiadiazines Anti-Inflammatory Agents Non-Steroidal Triazoles chemistry Female Lipid Peroxidation medicine.drug |
| Zdroj: | Archiv der Pharmazie. 342:291-298 |
| ISSN: | 1521-4184 0365-6233 |
| DOI: | 10.1002/ardp.200800188 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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