Journal of Medicinal Chemistry p. 604 - 609 (1981)
Update date:2022-08-05
Topics: Anti-Inflammatory Activity Experimental terms Acute Toxicity
Powers, Larry J.
Fogt, S. W.
Ariyan, Z. S.
Rippin, D. J.
Heilman, R. D.
Matthews, Richard J.
The effect of structural change on the biological activity of a series of imidazothiazoles and thiazolobenzimidazoles is described.It was found that compounds with polar substituents at the 2 or 3 position of the ring system are less acutely toxic while maintaining antiinflammatory activity.Other structural changes, such as the incorporation of a gem-dimethyl substituent in the 6 position, increase acute toxicity and eliminate antiinflammatory activity.The compound with the best activity/toxicity ratio contains an alkyl sulfonyl substituent on the thiazole ring.The thiazolobenzimidazole analogues are more potent than the imidazole analogues.
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(1981)