New cyclic butyrophenone derivatives in the indole series as potential atypical antipsychotics. A simple and practical synthesis of 6-aminomethyl-tetrahydroindol-4- …

CF Masaguer, E Raviña, I Loza, JA Fontenla

Index: Masaguer, Christian F.; Ravina, Enrique; Loza, Isabel; Fontenla, Jose Angel Bioorganic and Medicinal Chemistry Letters, 1997 , vol. 7, # 7 p. 913 - 918

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Citation Number: 13

Abstract

A simple and efficient synthesis of novel 6-aminomethyl-tetrahydroindol-4-ones, which are butyrophenone analogues of molindone, is described. These compounds exhibit potent affinities for D2 and 5-HT2A receptors in vitro. The most active compounds, 6d (QF 0408B) and 6e (QF 0409B), with pKi (5-HT2A/D2) ratios of 1.32 and 1.17 respectively, show an antipsychotic profile according to Meltzer's classification.

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