218933-36-9Relevant articles and documents
5HT7 receptor ligands and compositions comprising the same
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, (2010/03/02)
The present invention relates to compounds having pharmacological activity towards the 5-HT7 receptor, especially as agonists, identified by using a pharmacophore and a descriptor's profile filter as well as to pharmaceutical compositions comprising them. These compounds are useful in therapy in particular for the treatment and or prophylaxis of a disease in which 5-HT7 is involved, such as CNS disorders.
New generation dopaminergic agents. 5. Heterocyclic bioisosteres that exploit the 3-OH-N1-phneylpiperazine dopaminergic template
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.
, p. 2675 - 2680 (2007/10/03)
The synthesis of several bioisoteric 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.