Journal of Medicinal Chemistry p. 350 - 361 (1992)
Update date:2022-08-03
Topics:
Cullen, Ernest
Becker, Reinhold
Freter, Kurt
LeClerq, Thelma
Possanza, Genus
Wong, Hin-Chor
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.
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