Antithyroid drug carbimazole and its analogues: synthesis and inhibition of peroxidase-catalyzed iodination of L-tyrosine

Das, Debasis ; Roy, Gouriprasanna ; Mugesh, Govindasamy (2008) Antithyroid drug carbimazole and its analogues: synthesis and inhibition of peroxidase-catalyzed iodination of L-tyrosine Journal of Medicinal Chemistry, 51 (22). pp. 7313-7317. ISSN 0022-2623

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Official URL: http://pubs.acs.org/doi/abs/10.1021/jm800894m

Related URL: http://dx.doi.org/10.1021/jm800894m

Abstract

Synthesis and biological activity of the antithyroid drug carbimazole (CBZ) and its analogues are described. The introduction of an ethoxycarbonyl group in methimazole and its selenium analogue not only prevents the oxidation to the corresponding disulfide and diselenide but also reduces the zwitterionic character. A structure-activity correlation in a series of CBZ analogues suggests that the presence of a methyl substituent in CBZ and related compounds is important for their antithyroid activity.

Item Type:Article
Source:Copyright of this article belongs to American Chemical Society.
ID Code:79309
Deposited On:25 Jan 2012 06:33
Last Modified:25 Jan 2012 06:33

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