Bis basic substituted diaminobenzobisthiazoles as potential antiarthritic agents
| Autor: | Thelma LeClerq, Hin Chor Wong, Kurt Freter, Ernest Cullen, Reinhold Becker, Genus J. Possanza |
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| Rok vydání: | 1992 |
| Předmět: |
Male
Inflammation Hemolytic Plaque Technique Pharmacology chemistry.chemical_compound Mice Mice Inbred AKR Structure-Activity Relationship Drug Discovery medicine Animals Edema ED50 biology Molecular Structure Anti-Inflammatory Agents Non-Steroidal Biological activity Rats Inbred Strains medicine.disease Arthritis Experimental Carrageenan Rats Thiazoles chemistry Biochemistry Granuloma biology.protein Molecular Medicine Cyclooxygenase medicine.symptom Swelling Adjuvant arthritis |
| Zdroj: | Journal of medicinal chemistry. 35(2) |
| ISSN: | 0022-2623 |
| Popis: | A series of benzobisthiazoles were screened for antiinflammatory activity in the carrageenan paw edema and adjuvant arthritis tests. Compound 26, 2,6-bis(N,N-diethylamino)benzo[1,2-d:5,4-d']bisthiazole, was found to inhibit the swelling of the uninjected paw in the prophylactic adjuvant arthritis model with an ED50 of 2.3 mg/kg orally. As with most compounds of this series, 26 was inactive in acute model of inflammation, such as paw edema; like steroids, it showed activity in the granuloma pouch assay but did not inhibit cyclooxygenase, indicating a mode of action different from the classical nonsteroidal antiinflammatory drugs (NSAID's). At doses higher than those producing antiinflammatory activity, 26 had some immunoregulating properties. |
| Databáze: | OpenAIRE |
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