A new synthetic approach of N-(4-amino-2-methylquinolin-6-yl)-2-(4-ethylphenoxymethyl) benzamide (JTC-801) and its analogues and their pharmacological …

I Sestili, A Borioni, C Mustazza, A Rodomonte…

Index: Sestili, Isabella; Borioni, Anna; Mustazza, Carlo; Rodomonte, Andrea; Turchetto, Luciana; Sbraccia, Maria; Riitano, Daniela; Del Giudice, Maria Rosaria European Journal of Medicinal Chemistry, 2004 , vol. 39, # 12 p. 1047 - 1057

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Citation Number: 29

Abstract

A series of 4-amino-2-methylquinoline and 4-aminoquinazoline derivatives, including the reference NOP antagonist JTC-801, were synthesized by an alternative pathway and their in vitro pharmacological properties were investigated. 3-Substitution of the quinoline ring resulted very critical for affinity. So 3-methyl derivative 4j showed a similar potency compared with the reference 4h while bulky lipophilic or electron withdrawing groups in ...