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The activation of thyroid\u2010stimulating hormone (TSH) receptor by auto\u2010antibodies leads to \u2018<jats:italic>hyperthyroidism<\/jats:italic>\u2019, a life\u2010threatening disease which is treated by antithyroid drugs such as 6\u2010propyl\u20102\u2010thiouracil (PTU) and methimazole (MMI). The present review describes the biological activities of a number of S\/Se derivatives bearing the methimazole pharmacophore. It is shown that the isosteric substitutions in the existing drugs lead to compounds that can effectively and reversibly inhibit the heme\u2010containing lactoperoxidase (LPO). In contrast to methimazole, the selenium analogue, MSeI, does not interfere with the enzyme directly, but it inhibits LPO by reducing the H<jats:sub>2<\/jats:sub>O<jats:sub>2<\/jats:sub> that is required for the oxidation of the Fe\u2010center in LPO. These studies reveal that the degradation of the intracellular H<jats:sub>2<\/jats:sub>O<jats:sub>2<\/jats:sub> by the Se analogues of antithyroid drugs may be beneficial to the thyroid gland, as these compounds may act as antioxidants and protect thyroid cells from oxidative damage. Because the drugs with an action essentially on H<jats:sub>2<\/jats:sub>O<jats:sub>2<\/jats:sub> can reversibly inhibit the thyroid peroxidase, such drugs could be of great importance in the treatment of hyperthyroidism.<\/jats:p>","DOI":"10.1002\/cbdv.200890042","type":"journal-article","created":{"date-parts":[[2008,3,20]],"date-time":"2008-03-20T14:20:29Z","timestamp":1206022829000},"page":"414-439","source":"Crossref","is-referenced-by-count":38,"title":["Selenium Analogues of Antithyroid Drugs \u2013 Recent Developments"],"prefix":"10.1002","volume":"5","author":[{"given":"Gouriprasanna","family":"Roy","sequence":"first","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Govindasamy","family":"Mugesh","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"311","published-online":{"date-parts":[[2008,3,20]]},"reference":[{"key":"e_1_2_1_1_2","unstructured":"L.\u2005E. Ericson V. Johanson J. Molne M. 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