| 18603331 |
Zajdel P, Subra G, Verdie P, Bojarski AJ, Duszynska B, Basista K, Obniska J, Martinez J, Pawlowski M: The influence of an ethylene spacer on the 5-HT (1A) and 5-HT (2A) receptor affinity of arylpiperazine derivatives of amides with N-acylated amino acids and 3-differently substituted pyrrolidine-2,5-diones. Eur J Med Chem. 2009 Feb;44(2):800-8. Epub 2008 Jul 7.
A library of ethylene analogs of the previously described arylpiperazines with N-acylated amino acids was synthesized on SynPhase Lanterns and the library representatives were evaluated for their 5-HT (1A) and 5-HT (2A) receptor affinities. The obtained results were compared with those reported for compounds containing propylene and a butylene spacer and they revealed that 5-HT (1A) receptor affinity decreased proportionally with the length of the alkyl chain. Furthermore, the synthesized 3-cycloalkyl derivatives containing two methylene group spacers showed that the 3-position of pyrrolidine-2,5-dione preferred substituents of hydrophobic character. |
2(0,0,0,2) |