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

I van Wijngaarden, D Hamminga…

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

Full Text: HTML

Citation Number: 58

Abstract

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. ...

Related Articles:

An efficient one pot transfer hydrogenation and N-alkylation of quinolines with alcohols mediated by Pd/C/Zn

[Organic and Biomolecular Chemistry, , vol. 10, # 9 p. 1826 - 1833]

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

[Journal of Medicinal Chemistry, , vol. 36, # 23 p. 3693 - 3699]

An efficient one pot transfer hydrogenation and N-alkylation of quinolines with alcohols mediated by Pd/C/Zn

[Abarca, Belen; Adam, Rosa; Ballesteros, Rafael Organic and Biomolecular Chemistry, 2012 , vol. 10, # 9 p. 1826 - 1833]

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

[Journal of Medicinal Chemistry, , vol. 36, # 23 p. 3693 - 3699]

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

[Journal of Medicinal Chemistry, , vol. 36, # 23 p. 3693 - 3699]

More Articles...