Antithyroid substances. 1. The mercaptoglyoxalines

Searle, C. E.; Lawson, A. M.; Hemmings, A. W.

doi:10.1042/bj0470077

Cited by 19 publications

(13 citation statements)

References 8 publications

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“…Stanley and Astwood (1947), using in vivo counting and singledose technique, have assayed drugs for antithyroid activity in man. However, there has been little work on the correlation of results obtained using single or repeated doses and there is a general assumption that comparable results may be obtained by either method (Searle et al, 1950). The results of the present investigation on thiohydantoins do not support this assumption.…”

Section: Resultscontrasting

confidence: 55%

“…Searle et al (1950), using the single-dose technique, did not find any increase of activity with 4-alkyl substitution on 2-mercaptoglyoxaline, and they compared this with the results obtained by Astwood et al (1945) on chronic testing. Searle et al (1950) do not appear to have studied dose/response curves with all their 4-alkyl derivatives. It is possible that varying rates of metabolism or excretion may account for differences found between singledose testing and more chronic administration of compounds.…”

Section: Resultsmentioning

confidence: 99%

“…Alternatively, antithyroid activity is measured after a single dose of the test substance, using uptake of radioiodine (Larson, Keating, Peacock, and Rawson, 1945). Many compounds were tested in this way by McGinty et al (1948) and later by Searle et al (1950). These observers used experimental animals, and thyroidal radioiodide was measured on dissected thyroids.…”

Section: Resultsmentioning

confidence: 99%

“…A similar method was used by Searle, Lawson, and Hemmings (1950). Each substance was given in aqueous solution by stomach tube, in a dose of 0.05 m.mole/kg.…”

mentioning

confidence: 99%

“…Lewis (1913) reported some acute toxicity studies. Astwood, Bissell, and Hughes (1945), Jackman, Klenk, Fishburn, Tullar, and Archer (1948) and Searle, Lawson, and Morley (1951) included some thiohydantoin derivatives in the large number of compounds which they examined for antithyroid activity. Thiohydantoin is very similar structurally to thiouracil and mercaptoglyoxaline ( derivatives, like the parent compound, were found to have antithyroid activity.…”

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confidence: 99%

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Antithyroid Activity of Thiohydantoins

Kilpatrick

Elmore

Wood

1958

British Journal of Pharmacology and Chemotherapy

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The antithyroid activity of 2-thiohydantoin and some derivatives has been measured in rats, after a single dose and, also, after daily administration for 6 weeks. 2-Thiohydantoin and its 5-alkyl derivatives from 5-methyl to 5-sec-butyl-showed considerable antithyroid activity at a dose of 0.05 m.mole/kg. by mouth, but 5-n-hexyl-2-thiohydantoin had insignificant activity at this dose level. The presence of polar groups in the 5-substituent was associated with reduction or complete loss of activity. By the single-dose technique, 2-thiohydantoin was more potent than its 5-alkyl derivatives. The opposite result was obtained by other methods of assessment after 42 days of treatment. Some of the possible factors involved are discussed especially in relation to the difficulty of comparing results obtained by the different methods of assessment. The acute toxicity of 2-thiohydantoin and of its 5-methyl and 5-ethyl derivatives is reported. No toxic effects were found after daily administration of several 2-thiohydantoins at a dose of 50 mg./kg. for 6 weeks.

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Section: Resultscontrasting

confidence: 55%

Section: Resultsmentioning

confidence: 99%

Section: Resultsmentioning

confidence: 99%

“…A similar method was used by Searle, Lawson, and Hemmings (1950). Each substance was given in aqueous solution by stomach tube, in a dose of 0.05 m.mole/kg.…”

mentioning

confidence: 99%

mentioning

confidence: 99%

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