Synthesis, Testing and Structure-Activity Studies on a Library of 5-HT4 Ligands

A Hanna-Elias, DT Manallack, A Levit…

Index: Hanna-Elias, Amir; Manallack, David T.; Levit, Alla; Nguyen, William; Ayad, Fadi; Perera, Glen; Shapiro, Marina; Irving, Helen R.; Coupar, Ian M.; Iskander, Magdy N. Medicinal Chemistry, 2010 , vol. 6, # 6 p. 344 - 354

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Abstract

Several indole derivatives and analogues comprising a range of related structural classes were designed, synthesized and tested as ligands for the 5-HT4 receptor. Within each series, binding experiments showed compounds with good affinity demonstrating high percentage displacement values at 1 αM. The most potent of these (20) had a pKi of 8.54 demonstrating very good affinity. These indole analogues were combined with 55 ligands ...