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J Med Chem ; 35(2): 350-61, 1992 Jan 24.
Article in English | MEDLINE | ID: mdl-1732553

ABSTRACT

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.


Subject(s)
Anti-Inflammatory Agents, Non-Steroidal/chemical synthesis , Thiazoles/chemical synthesis , Animals , Anti-Inflammatory Agents, Non-Steroidal/chemistry , Anti-Inflammatory Agents, Non-Steroidal/pharmacology , Arthritis, Experimental/drug therapy , Edema/drug therapy , Hemolytic Plaque Technique , Male , Mice , Mice, Inbred AKR , Molecular Structure , Rats , Rats, Inbred Strains , Structure-Activity Relationship , Thiazoles/chemistry , Thiazoles/pharmacology
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