| Autor: |
Leach CA; SmithKline Beecham Pharmaceuticals R&D, Welwyn, Herts, England., Brown TH, Ife RJ, Keeling DJ, Laing SM, Parsons ME, Price CA, Wiggall KJ |
| Jazyk: |
angličtina |
| Zdroj: |
Journal of medicinal chemistry [J Med Chem] 1992 May 15; Vol. 35 (10), pp. 1845-52. |
| DOI: |
10.1021/jm00088a021 |
| Abstrakt: |
Further work on compounds 1 has identified the 4-position as a site where substantial modifications are tolerated, leading to analogues which are more potent and less toxic than those described previously. The best compound in the series is 13a (SK&F 96356), which is a potent inhibitor of gastric acid secretion in both the pentagastrin-stimulated rat and the histamine-stimulated dog. This compound shows reversible, K(+)-competitive binding to the enzyme. Because of its fluorescent properties, it is also proving useful in vitro as a probe of the structure and function of the (H+/K+)-ATPase. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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