New generation dopaminergic agents. 5. Heterocyclic bioisosteres that exploit the 3-OH-N 1-phenylpiperazine dopaminergic template

…, GB McGaughey, JA Nelson, H Mazandarani…

文献索引：Mewshaw, Richard E.; Verwijs, Antoine; Shi, Xiaojie; McGaughey, Georgia B.; Nelson, James A.; Mazandarani, Hossein; Brennan, Julie A.; Marquis, Karen L.; Coupet, Joseph; Andree, Terrance H. Bioorganic and Medicinal Chemistry Letters, 1998 , vol. 8, # 19 p. 2675 - 2680

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被引用次数: 6

摘要

The synthesis of several bioisosteric analogs based on the 3-OH-N1-phenylpiperazine dopamine D2 agonist template (ie, 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.