Synthesis, anti-inflammatory, analgesic and antioxidant activities of some tetrasubstituted thiophenes
| Autor: | Madhubhai M. Patel, Mustakim Mansuri, Navedul Haque, Khurshid I. Molvi, Syed Muzaffar A. Andrabi, V. Sudarsanam |
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| Rok vydání: | 2008 |
| Předmět: |
Male
Antioxidant medicine.drug_class medicine.medical_treatment Anti-Inflammatory Agents Thiophenes Anti-inflammatory Antioxidants chemistry.chemical_compound Acetic acid Structure-Activity Relationship Chloroacetone In vivo Drug Discovery medicine Organic chemistry Animals Pharmacology Inflammation Analgesics Molecular Structure Chemistry General Medicine Coumarin Ibuprofen Ascorbic acid Rats Female Nuclear chemistry medicine.drug |
| Zdroj: | Journal of enzyme inhibition and medicinal chemistry. 23(6) |
| ISSN: | 1475-6374 |
| Popis: | Sets of tetrasubstituted thiophene esters 4a-4g, 5a-5f and 6a-6e were synthesized by reaction of 1-(alpha-Carbomethoxy-beta-aminothiocrotonoyl)-aryl/aroyl amines (3) with 3-(bromoacetyl)coumarin, 1,4-dibromodiacetyl and chloroacetone respectively. The compound 3 were synthesized by nucleophilic addition of aryl/aroylisothiocyanate and enamine (2). The synthesized targeted compounds (4a-4g, 5a-5f and 6a-6e) were evaluated for their in vivo anti-inflammatory activity in carrageenin-induced rat hind paw oedema model at three graded doses employed at 10, 20 and 40 mg/kg body weight using mefanamic acid, ibuprofen and in vivo analgesic activity in acetic acid induced writhing response model at 10 mg/kg dose using ibuprofen as standard drug. The compounds 4a-4f, 5c, 5f, 6c and 6e were evaluated for their in vitro antioxidant nitric oxide radical scavenging assay at the concentrations of 5, 10, 15, 20, 25, 30 and 35 microg/mL using ascorbic acid as standard drug. Among all the targeted compounds 4c showed maximum anti-inflammatory activity of 71% protection at 10 mg/kg and 77% protection at 20 mg/kg to inflamed paw and analgesic activity of 56% inhibition and also maximum in vitro nitric oxide radical scavenging activity having IC(50) value 31.59 microg/mL. |
| Databáze: | OpenAIRE |
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