ISSN:
0018-019X
Keywords:
Chemistry
;
Organic Chemistry
Source:
Wiley InterScience Backfile Collection 1832-2000
Topics:
Chemistry and Pharmacology
Notes:
The structures of the essential metabolites which are excreted by the rat after oral application of GS 13005 (O,O-dimethyl-S-[(2-methoxy-1,3,4-thiadiazole-5(4H)-one-4-yl)-methyl] dithiophosphate) have been elucidated. The product of final oxidation, CO2, was found to be the main metabolite (up to 36% of the dose applied). Among the degradation products excreted in the urine (up to 45% of the dose applied) the two most important were isolated. They are 4-methylsulfinylmethyl and 4-methylsulfonylmethyl derivatives respectively of the intact 2-methoxy-1,3,4-thiadiazole-5-one heterocycle (metabolites III and II, in amounts of 20-25% and 5-7% of the dose applied, respectively). These metabolites originate by methylation and subsequent oxidation from the mercaptomethyl derivative liberated after hydrolysis of the P—S bond of the dithiophosphoric acid ester.
Additional Material:
2 Ill.
Type of Medium:
Electronic Resource
URL:
http://dx.doi.org/10.1002/hlca.19680510313
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