title: Synthesis and sar of 2- and 3-substituted 7-azaindoles as potential dopamine D4 ligands.
abstract: 7-azaindole compounds bearing a cyclic amine moiety linked by a one or two carbon chain attached at the 2- or 3-position were synthesised and evaluated as potential dopamine D4 ligands. Highest affinity and selectivity for the D4 receptor resided in the 3-aminomethyl-7-azaindole series.
authors: Department of Medicinal Chemistry, Merck Sharp & Dohme Research Laboratories, Neuroscience Research Centre, Harlow, Essex, UK. Neil_Curtis@Merck.com
authors: N R
authors: NR
authors: Curtis
authors: J J
authors: JJ
authors: Kulagowski
authors: P D
authors: PD
authors: Leeson
authors: M P
authors: MP
authors: Ridgill
authors: F
authors: F
authors: Emms
authors: S B
authors: SB
authors: Freedman
authors: S
authors: S
authors: Patel
authors: S
authors: S
authors: Patel
mesh_terms: D001372:Aza Compounds / Q000737:chemistry*; D006801:Humans; D007211:Indoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism; D008024:Ligands; D015394:Molecular Structure; D011485:Protein Binding; D017448:Receptors, Dopamine D2 / Q000378:metabolism*; D050638:Receptors, Dopamine D4; D013329:Structure-Activity Relationship
chemical_list: D001372:Aza Compounds; C493599:DRD4 protein, human; D007211:Indoles; D008024:Ligands; D017448:Receptors, Dopamine D2; D050638:Receptors, Dopamine D4