5-Substituted 1H-pyrrolo[3,2-b]pyridines as inhibitors of gastric acid secretion☆
2007; Elsevier BV; Volume: 16; Issue: 3 Linguagem: Inglês
10.1016/j.bmc.2007.10.017
ISSN1464-3391
AutoresAndreas Marc Palmer, Gabriela Münch, Christof Brehm, Peter Jan Zimmermann, Wilm Buhr, Martin P. Feth, Wolfgang Simon,
Tópico(s)Asymmetric Synthesis and Catalysis
ResumoA 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.
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