Structure-affinity relationship study on N-[4-(4-arylpiperazin-1-yl)butyl]arylcarboxamides as potent and selective dopamine D(3) receptor ligands.

@article{Leopoldo2002StructureaffinityRS,
  title={Structure-affinity relationship study on N-[4-(4-arylpiperazin-1-yl)butyl]arylcarboxamides as potent and selective dopamine D(3) receptor ligands.},
  author={Marcello Leopoldo and Francesco Berardi and Nicola A. Colabufo and Paola De Giorgio and Enza Lacivita and Roberto Perrone and Vincenzo Tortorella},
  journal={Journal of medicinal chemistry},
  year={2002},
  volume={45 26},
  pages={5727-35}
}
The benzamide PB12 (N-[2-[4-(4-chlorophenyl)piperazin-1-yl]ethyl]-3-methoxybenzamide) (1), already reported as potent and selective dopamine D(4) receptor ligand, has been modified searching for structural features that could lead to D(3) receptor affinity. Changes in the aromatic ring linked to N-1 piperazine ring led to the identification of 2-methoxyphenyl and 2,3-dichlorophenyl derivatives (compounds 6 and 13) displaying moderate D(3) affinity (K(i) = 145 and 31 nM, respectively… CONTINUE READING

From This Paper

Topics from this paper.
11 Citations
0 References
Similar Papers

Citations

Publications citing this paper.
Showing 1-10 of 11 extracted citations

Similar Papers

Loading similar papers…