Development of high-affinity 5-HT3 receptor antagonists. Structure-affinity relationships of novel 1, 7-annulated indole derivatives. 1

I van Wijngaarden, D Hamminga…

文献索引：Van Wijngaarden; Hamminga; Van Hes; Standaar; Tipker; Tulp; Mol; Olivier; De Jonge Journal of Medicinal Chemistry, 1993 , vol. 36, # 23 p. 3693 - 3699

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被引用次数: 58

摘要

On the basis of the structures of ondansetron and GR 65,630, its ring-opened Winked methylimidazole analogue, novel 1, 7-annelated indole derivatives were synthesized as potential 5-HT3 antagonists. Receptor binding studies show that all compounds display a high affinity for the 5-HT3 receptors. In both series annelation results in compounds being 7 and 4 times more potent than the references ondansetron and GR 65,630, respectively. ...