• Bulletin of the Korean Chemical Society
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• v.31 no.11
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• pp.3073-3074
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• 2010

• Bulletin of the Korean Chemical Society
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• v.31 no.11
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• pp.3318-3326
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• 2010

Five new series of 3,4-ethylenedioxythiophene derivatives carrying important pharamacophores, viz., amide, ester, ether and active secondary aryl moieties have been designed and synthesized through multistep reactions starting from thiodiglycolic ester and diethyl oxalate. They have been characterized by elemental and spectral data. All the target compounds have been screened for their anticonvulsant activity at three different models viz. maximal electroshock (MES), subcutaneous metrazole (scMET), and 6 Hz screen and evaluated for their neurotoxicity in rotorod model. Compound 6a emerged as lead with no neurotoxicity. All the five series of compounds are safe in the toxicity studies at the maximum dose of 300 mg/kg of body weight. Amongst the tested compounds, the ester pharmacophore with thioamide fragment has showed better activity than the other analogs.

• Bulletin of the Korean Chemical Society
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• v.25 no.6
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• pp.779-785
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• 2004

Syn (or anti) cinnamaldehydeoxime (1a, b) undergoes Diels-Alder addition to tetrabromo-p-benzoquinone (2)in dry xylene in 1 : 1 and 2 : 1 molar ratios to give the mono- and diadducts 3 and 4a, b respectively. The reaction of 3 with thioamides in ethanol gave thiazoloquinoline diones 6a-d, whereas with acid amides in ethylene glycol, it gave oxazoloquinolinediones 12a-f.

• The Korean Journal of Nuclear Medicine
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• v.11 no.1
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• pp.49-58
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• 1977

For the assessment of antithyroid effect of lithium carbonate, it was administered to the 17 hyperthyroid and 5 euthyroid patients, who visited the Seoul National University Hospital from Jan. to Aug., 1977. Thyroid function tests were performed just before the administration of Lithium carbonate, 2 weeks and 2 months after lithium treatment. The results were as follows; 1) In the 5 euthyroid patients, no significant changes in thyroid function tests were obtained before and after lithium treatment. 2) In the 17 hyperthyroid patients, the values of the $T_3RIA$ were $370{\pm}121ng/dl$ 2 weeks after lithium treatment as compared with $506{\pm}121ng/dl$ before the administration, of which the mean percentage fall was 26.9%. $T_3RU$ was varied from $56.8{\pm}8.0%\;to\;47.3{\pm}8.1%$ (16.7% in mean percentage fall), $T_4$ was changed from $24.2{\pm}2.4ug/dl\;to\;22.0{\pm}4.2ug/dl$ (9.1% in mean fall), and $T_7$, from $13.82{\pm}2.25\;to\;10.55{\pm}3.12$ (23.7% in mean fall). 3) In the 5 hyperthyroid patients, serial thyroid function tests were performed 2 weeks and 2 months later. The mean percentage falls of $T_3RIA$ were 36.6 and 61.3%, 2 weeks and 2 months after lithium treatment respectively. Those of $T_3RU$ were 17.5 and 35.1%, those of $T_4$ were 20.4 and 44.0%, $T_7$, 35.0 and 60.7%. 4) Approximately $45{\sim}60%$ of mean fall in thyroid function tests were obtained within the second week. Normal thyroid function tests were observed in 2 among 17 patients within the second week, and 2 among 5 patients within the second month. 18 patients, however, became clinically euthyroid within the 4th week. 5) Single case of hypothyroidism was experienced, and 5 patients (29.4%) complained mild side effects. Lithium salts could be safely administered to hyperthyroid patients who are allergic to thioamides or iodine. Its use is indicated in cases of acute thyrotoxicosis in which it's necessary to reduce hormone levels very rapidly, and lithium-thioamides drug combination is a highly effective and safe means of initial routine control of hyperthyroidism.