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Lee JH, Choi YH, Lim YJ, Lee BS, Chi DY, Jin C: Syntheses and binding affinities of 6-nitroquipazine analogues for serotonin transporter. Bioorg Med Chem. 2007 May 15;15(10):3499-504. Epub 2007 Mar 3.
Part 5: 2'-Substituted 6-nitroquipazines.. Five C2'-substituted 6-nitroquipazine (6-NQ) derivatives were prepared and evaluated in terms of their biological abilities (K (i)) to displace [(3) H] citalopram binding to serotonin transporter. The relationship between their structure and biological activities revealed that shorter alkyl groups tend to possess higher binding affinity. Both compounds 12a and 12c were found to have the equally highest binding affinity (K (i)=0.43+/-0.02 nM). |
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