Renin inhibitory pentols showing improved enteral bioavailability
| Autor: | H W, Kleemann, H, Heitsch, R, Henning, W, Kramer, W, Kocher, U, Lerch, W, Linz, W U, Nickel, D, Ruppert, H, Urbach |
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| Rok vydání: | 1992 |
| Předmět: |
Male
Lactams Brush border Biological Availability Blood Pressure Pharmacology Enteral administration Structure-Activity Relationship Sugar Alcohols In vivo Intestine Small Renin Drug Discovery Renin–angiotensin system Animals Humans Enzyme Inhibitors biology Chemistry Vesicle Amino Sugars Biological activity Macaca mulatta Anti-Bacterial Agents Bioavailability Solubility Biochemistry Enzyme inhibitor biology.protein Molecular Medicine Female Rabbits |
| Zdroj: | Journal of Medicinal Chemistry. 35:559-567 |
| ISSN: | 1520-4804 0022-2623 |
| DOI: | 10.1021/jm00081a019 |
| Popis: | Incorporation of a C-terminal pentahydroxy functionality led to potent, low molecular weight hydrophilic renin inhibitors lacking the P1' side chain. As these compounds are easy to synthesize and have sufficient water solubility, they were chosen for further study. Compound 33 was transported across rabbit intestinal brush border membrane vesicles and yielded a hypotensive effect in sodium-depleted rhesus monkeys which lasted for 90 min when dosed at 2 mg/kg id. |
| Databáze: | OpenAIRE |
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