New carriers for representative peptides and peptide drugs

被引:15
作者
Aboul-Fadl, T [1 ]
El-Shorbagi, AN [1 ]
机构
[1] Univ Assiut, Fac Pharm, Assiut 71526, Egypt
关键词
tetrahydro-2H-1,3,5-thiadiazine-2-thione; glycylglycine; prodrugs; lipophilicity; hydrolysis kinetics;
D O I
10.1002/ardp.19973301103
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
3,5-Disubstituted tetrahydro-2H-1,3,5-thiadiazine-2-thione (THTT) derivatives; 4a-g were prepared and found to be a promising prodrug approach for peptide drugs. The pH profile for-their degradation in aqueous buffer solutions was determined using HPLC technique and accounted for, in terms of specific base-catalyzed reactions. All of the compounds however, showed high acid-stability. Enzymatic (human serum) hydrolysis of the different derivatives offered an advantageous range of t(1/2)'s; the property that hermits controlling onset and duration of actions of drugs.
引用
收藏
页码:327 / 332
页数:6
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