European Journal of Medicinal Chemistry p. 11 - 16 (1994)
Update date:2022-08-05
Topics:
El-Shorbagi, A-Na
Phenethylamine 1a (a; n = 2) and benzylamine 1b (b; n = 1) are known in medicinal chemistry as strong vasopressors.Both are excellent substrates for the enzyme monoamine oxidase (MAO).The 2 compounds were incorporated in a highly lipid-soluble and hydrolysis-vulnerable tetrahydrothiadiazine (THTT) target structure in order to modify their pharmacokinetics.Better partition correlations, expressed as log P (calculated and observed) for the synthesized products THTT in comparison to the original compounds 1a,b have been found.One of the THTT derivatives was tested for its liability for chemical hydrolysis and the structure of the hydrolytic product was determined. tetrahydro-2H-1,3,5-thiadiazine-2-thione / phenethylamine / benzylamine / prodrugs / monoamine oxidase inhibitors / partition coefficient / hydrolysis
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