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Abstract

The E-state approach provides guidelines to economize efforts and cost of designing new antithyroid drugs.

Liquid chromatographic assay of abouthiouzine in plasma and its application to pharmacokinetic studies

“…Abouthiouzine was designed using electrotopologicalstate (E-state) indexes and synthesized in the college of Pharmacy's research laboratories (King Saud University, Riyadh, Saudi Arabia), as it has previously been described [3,4]. Propranolol was purchased from Sigma (St. Louis, MO, USA); methanol, acetonitrile, and ethyl acetate of HPLC grade were obtained from BDH Laboratory (BDH Chemicals Ltd., Poole, UK).…”

“…(Fig. 1) is a newly designed antithyroid agent with a reportedly less side effects profile compared to other drugs used in the treatment of hyperthyroidism [3]. The relative efficacy of abouthiouzine, after equimolar dose, was found to be 102% and 51.5% of that of propylthiouracil with respect to the rate of 125 l-discharge and 125 l-uptake, respectively.…”

“…The relative efficacy of abouthiouzine, after equimolar dose, was found to be 102% and 51.5% of that of propylthiouracil with respect to the rate of 125 l-discharge and 125 l-uptake, respectively. In addition, chemiluminescence studies on polymorphonuclears (PMNs) revealed that abouthiouzine has only slight oxidant property [3]. Such properties may provide advantages in avoiding the iatrogenic hypothyroidism and antithyroid-induced immunological reactions.…”

Synthesis of Some Novel Derivatives of 2-(9H-purin-6-ylsulfanyl) Acetohydrazide as Potential Antithyroid Agents

“…The widely used synthetic antithyroid agents (SATs) like propylthiouracil, methimazole and carbimazole belong to sulfonamide group and have serious side effects [3]. Keeping in view the scarcity and side effects of the existing drugs, many compounds were evaluated and some were reported to possess recognizable antithyroid activity [4]. It has been observed that compounds capable of making stable charge transfer complex with iodine and having formation constant (K c ) values ≥100 L mol -1 generally exhibit antithyroid effects in vivo [5].…”

Antithyroid activity of some 6-(alkylsulfanyl)-9H-purines

“…2 On the other hand, surgery may lead to tracheal compression due to bleeding, infection, bilateral vocal fold paralysis and superior laryngeal nerve damage. 5,10 SATs are supposed to act either through inhibition of the thyroperoxidase enzyme or by making stable charge transfer (CT) complexes with iodine in which iodine acts as a σ-acceptor and the synthetic compound as an n-donor. 3,4 Moreover, certain hyperthyroid conditions are not permanent and do not need surgery or radioiodine therapy.…”