Syntheses and binding affinities of 6-nitroquipazine analogues for serotonin transporter. Part 2: 4-substituted 6-nitroquipazines

BS Lee, S Chu, BS Lee, DY Chi, YS Song…

Index: Se Lee, Byoung; Chu, Soyoung; Lee, Bon-Su; Yoon Chi, Dae; Song, Yun Seon; Jin, Changbae Bioorganic and Medicinal Chemistry Letters, 2002 , vol. 12, # 5 p. 811 - 815

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Citation Number: 22

Abstract

Eleven 4-substituted derivatives of 6-nitroquipazine were synthesized and evaluated for their abilities to displace [3H] citalopram binding to the rat cortical synaptic membranes. Among them, 4-chloro-6-nitroquipazine was shown to possess the highest binding affinity (Ki= 0.03 nM) which was approximately 6 times higher than that of 6-nitroquipazine (Ki= 0.17 nM) itself. In this paper, we describe the syntheses of 4-substituted 6-nitroquipazine ...