Bioorganic & medicinal chemistry

Syntheses and binding affinities of 6-nitroquipazine analogues for serotonin transporter. Part 4: 3-Alkyl-4-halo-6-nitroquipazines

BS Moon, BS Lee, DY Chi

文献索引：Byung, Seok Moon; Byoung, Se Lee; Dae, Yoon Chi Bioorganic and Medicinal Chemistry, 2005 , vol. 13, # 16 p. 4952 - 4959

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被引用次数: 7

摘要

On the basis of the structure–activity relationship (SAR) of 4-chloro-6-nitroquipazine (Ki= 0.03 nM) and 3-fluoropropyl-6-nitroquipazine (Ki= 0.32 nM), 3-alkyl-4-halo-6-nitroquipazines were synthesized and tested for their potential abilities in vitro to displace [3H] citalopram binding to the rat cortical membranes. Binding affinities of 3b and 4d were Ki= 2.70±0.32 and 2.23±0.46 nM, respectively. The syntheses of 3-alkyl-4-halo-6-nitroquipazine, their in ...