Antithyroid Drug Carbimazole and Its Analogues: Synthesis and Inhibition of Peroxidase-Catalyzed Iodination of L-Tyrosine

Das, Debasis and Roy, Gouriprasanna and Mugesh, Govindasamy (2008) Antithyroid Drug Carbimazole and Its Analogues: Synthesis and Inhibition of Peroxidase-Catalyzed Iodination of L-Tyrosine. In: Journal of Medicinal Chemistry, 51 (22). pp. 7313-7317.

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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:	Journal Article
Publication:	Journal of Medicinal Chemistry
Publisher:	American Chemical Society
Additional Information:	Copyright of this article belongs to American Chemical Society.
Department/Centre:	Division of Chemical Sciences > Inorganic & Physical Chemistry
Date Deposited:	01 May 2009 08:59
Last Modified:	19 Sep 2010 04:57
URI:	http://eprints.iisc.ac.in/id/eprint/17562

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