Syntheses and binding affinities of 6-nitroquipazine analogues for serotonin transporter. Part 5: 2'-Substituted 6-nitroquipazines |
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Authors: | Lee Jae Hak Choi Yong Hyun Lim Yoo Jin Lee Byoung Se Chi Dae Yoon Jin Changbae |
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Affiliation: | Department of Chemistry, Inha University, 253 Yonghyundong, Namgu, Inchon 402-751, Republic of Korea. |
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Abstract: | 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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