Synthesis and sar of 2- and 3-substituted 7-azaindoles as potential dopamine D4 ligands

N R Curtis; J J Kulagowski; P D Leeson; M P Ridgill; F Emms; S B Freedman; S Patel; S Patel

doi:10.1016/s0960-894x(99)00025-6

Synthesis and sar of 2- and 3-substituted 7-azaindoles as potential dopamine D4 ligands

Bioorg Med Chem Lett. 1999 Feb 22;9(4):585-8. doi: 10.1016/s0960-894x(99)00025-6.

Authors

N R Curtis¹, J J Kulagowski, P D Leeson, M P Ridgill, F Emms, S B Freedman, S Patel, S Patel

Affiliation

¹ Department of Medicinal Chemistry, Merck Sharp & Dohme Research Laboratories, Neuroscience Research Centre, Harlow, Essex, UK. Neil_Curtis@Merck.com

PMID: 10098669
DOI: 10.1016/s0960-894x(99)00025-6

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.

MeSH terms

Aza Compounds / chemistry*
Humans
Indoles / chemical synthesis*
Indoles / chemistry
Indoles / metabolism
Ligands
Molecular Structure
Protein Binding
Receptors, Dopamine D2 / metabolism*
Receptors, Dopamine D4
Structure-Activity Relationship

Substances

Aza Compounds
DRD4 protein, human
Indoles
Ligands
Receptors, Dopamine D2
Receptors, Dopamine D4