4-Aminoethylpiperazinyl aryl ketones with 5-HT₁A/5-HT₇ selectivity.

@article{Kim20124AminoethylpiperazinylAK,
  title={4-Aminoethylpiperazinyl aryl ketones with 5-HT₁A/5-HT₇ selectivity.},
  author={Mi Kyoung Kim and Hyo Seon Lee and Sora Kim and Suh Young Cho and Bryan L. Roth and Youhoon Chong and Hyunah Choo},
  journal={Bioorganic & medicinal chemistry},
  year={2012},
  volume={20 2},
  pages={1139-48}
}
The well-known 5-HT(1A)/5-HT(7) selectivity issue was tackled by a new series of 4-aminoethylpiperazinyl aryl ketones (1a-1l) specifically designed to distinguish the two hydrophobic sites centered at the anchoring salt bridge. The 4-aminoethylpiperazinyl aryl ketones showed a wide spectrum of activity and selectivity for the 5-HT receptors depending on the type of the hydrophobic groups attached at the aryl piperazinyl ketone scaffold. Docking study of the most active compounds against 5-HT(7… CONTINUE READING