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The influence of groups in the molecule of 3 - keto - 2:3 - dihydrobenz - 1:4 - thiazine on its “antheimintic” properties

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RaeburnJ_1951redux.pdf (16.29Mb)
Date
1951
Author
Raeburn, John
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Abstract
 
 
It may be concluded that 3-keto-2:3-dihydrobenz-1:4-thiazine and its derivatives, with the exception of the unsubstituted compound itself and the 6-nitroso-derivative both of which have a slight stimulant effect, have no effect on the 'intermediate' preparations of Ascaris.
 
All but six, namely the 6-arsonic and stibonic acids, the 6-mercuric chloride compound, the 6-amino compound coupled with phloroglucinol and salicylic acid, and 6:6'-bis-(3-keto-2:3-dihydrobenz-1:4-thiazine), have a paralysant effect on liver fluke, the 6-amino and 6-thiol compounds being almost lethal at a concentration of 1 in 1000.
 
We may, therefore, conclude that certain atoms or groups increase the activity, whilst others decrease the activity of 3-keto-2:3-dihydrobenz-1:4-thiazinne towards liver fluke. The inactivity towards Ascaris may be partly due to the inability of the compounds to penetrate the Ascaris cuticle, a difficulty which it might be possible to overcome by using a suitable wetting agent.
 
URI
http://hdl.handle.net/1842/33610
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