5-Substituted 1H-pyrrolo[3,2-b]pyridines as inhibitors of gastric acid secretion
| Autor: | Christof Brehm, Wolfgang Alexander Simon, Peter Jan Zimmermann, Wilm Buhr, Martin Feth, Andreas Palmer, Gabriela Münch |
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| Rok vydání: | 2007 |
| Předmět: |
Stereochemistry
Pyridines Clinical Biochemistry Pharmaceutical Science H(+)-K(+)-Exchanging ATPase Biochemistry Chemical synthesis Catalysis Gastric Acid Structure-Activity Relationship Drug Discovery Gastric mucosa medicine Structure–activity relationship Animals Pyrroles Molecular Biology chemistry.chemical_classification Molecular Structure Organic Chemistry medicine.anatomical_structure Enzyme chemistry Gastric Mucosa Lipophilicity Molecular Medicine Gastric acid Rabbits |
| Zdroj: | Bioorganicmedicinal chemistry. 16(3) |
| ISSN: | 1464-3391 |
| Popis: | A series of novel 1H-pyrrolo[3,2-b]pyridines was prepared relying on a copper iodide catalyzed cyclization of 2-prop-1-ynylpyridin-3-amines. A structure-activity relationship was established focusing on the influence of the substitution pattern in position 1, 3, and 5 of the heterocycle on anti-secretory activity, lipophilicity, and pK(a) value. Some of the compounds proved to be potent inhibitors of the gastric acid pump. |
| Databáze: | OpenAIRE |
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