Effect of Structural Change on Acute Toxicity and Antiinflammatory Activity in a Series of Imidazothiazoles and Thiazolobenzimidazoles
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.
Powers, Larry J.,Fogt, S. W.,Ariyan, Z. S.,Rippin, D. J.,Heilman, R. D.,Matthews, Richard J.
p. 604 - 609
(2007/10/02)
Antiinflammatory imidazothiazoles and thiazolopyrimidines
Certain imidazothiazoles and thiazolopyrimidines have been found to prevent and inhibit the formation of granuloma tissue in animals. This result is accomplished by administering to the animal subject a therapeutically effective amount of a compound havin
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(2008/06/13)
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