Tranexamic acid derivatives with enhanced absorption
| Autor: | C. M. Svahn, F. Merenyi, Grälls M, L. Karlson, L. Widlund |
|---|---|
| Rok vydání: | 1986 |
| Předmět: |
Male
Acylal Antifibrinolytic Cyclohexanecarboxylic Acids Hydrochloride medicine.drug_class Rats Inbred Strains Absorption (skin) Cyclohexanecarboxylic acid Prodrug Rats Structure-Activity Relationship chemistry.chemical_compound Hydrolysis Intestinal Absorption Tranexamic Acid chemistry Drug Discovery medicine Animals Molecular Medicine Organic chemistry Tranexamic acid Nuclear chemistry medicine.drug |
| Zdroj: | Journal of Medicinal Chemistry. 29:448-453 |
| ISSN: | 1520-4804 0022-2623 |
| Popis: | Derivatives of the antifibrinolytic drug tranexamic acid [trans-4-(aminomethyl)cyclohexanecarboxylic acid] containing one or two tranexamic acid moieties were synthesized. Most of the derivatives have good stability in acidic and neutral solutions but are easily hydrolyzed in plasma. By measuring the amount of tranexamic acid excreted in the urine after an oral dose, relative absorptions of a number of derivatives in the rat were estimated. Most of the derivatives showed greater absorption than tranexamic acid itself. 1-[(Ethoxycarbonyl)oxy]ethyl trans-4-(amino-methyl)cyclohexanecarboxylate hydrochloride was chosen for studies in man. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
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