European journal of medicinal chemistry

Model for delivery of amines through incorporation into a tetrahydro-2H-1, 3, 5-thiadiazine-2-thione structure

ANA El-Shorbagi

文献索引：El-Shorbagi, A-Na European Journal of Medicinal Chemistry, 1994 , vol. 29, # 1 p. 11 - 16

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被引用次数: 19

摘要

Abstract 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 ...