Author/Authors :
Richard E. Mewshaw، نويسنده , , Antoine Verwijs، نويسنده , , Xiaojie Shi، نويسنده , , Georgia B. McGaughey، نويسنده , , James A. Nelson، نويسنده , , Hossein Mazandarani، نويسنده , , Julie A. Brennan، نويسنده , , Karen L. Marquis، نويسنده , , Joseph Coupet، نويسنده , , Terrance H. Andree، نويسنده ,
Abstract :
The synthesis of several bioisosteric analogs based on the 3-OH-N1-phenylpiperazine dopamine D2 agonist template (i.e., 4) is described. The indolone (5) and 2-CF3-benzimidazole (13) were observed to have excellent affinity for the D2 receptor. Several D4 selective compounds were also identified. Molecular modeling studies and a putative bioactive conformation are discussed.
