Synthesis, in vitro binding studies and docking of long-chain arylpiperazine nitroquipazine analogues, as potential serotonin transporter inhibitors

…, R Abagyan, AJ Bojarski, I Sylte, Z Chilmonczyk

Index: Jaronczyk, Malgorzata; Wolosewicz, Karol; Gabrielsen, Mari; Nowak, Gabriel; Kufareva, Irina; Mazurek, Aleksander P.; Ravna, Aina W.; Abagyan, Ruben; Bojarski, Andrzej J.; Sylte, Ingebrigt; Chilmonczyk, Zdzislaw European Journal of Medicinal Chemistry, 2012 , vol. 49, p. 200 - 210

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Citation Number: 3

Abstract

It is well known that 6-nitroquipazine exhibits about 150-fold higher affinity for the serotonin transporter (SERT) than quipazine and recently we showed quipazine buspirone analogues with high to moderate SERT affinity. Now we have designed and synthesized several 6- nitroquipazine buspirone derivatives. Unexpectedly, their SERT binding affinities were moderate, and much lower than that of the previously studied quipazine buspirone ...