Buspirone analogues. 2. Structure-activity relationships of aromatic imide derivatives.

  title={Buspirone analogues. 2. Structure-activity relationships of aromatic imide derivatives.},
  author={Jeff New and J P Yevich and Michael S. Eison and Duncan P. Taylor and Arlene Stark Eison and L. A. Riblet and Cam Vandermaelen and Daniel Temple},
  journal={Journal of medicinal chemistry},
  volume={29 8},
Several analogues of the novel anxiolytic buspirone were synthesized and evaluated in vivo for tranquilizing activity and their ability to reverse neuroleptic-induced catalepsy. The in vitro binding affinities of these compounds were also examined for both the alpha 1 and dopamine D2 receptor systems. The general structure-activity relationships of this series highlight compounds 17, 21, and 32 as having anticonflict activity. Each of these structures contains the 1-(2-pyrimidinyl)piperazine… CONTINUE READING


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