Design, synthesis and dopamine D4 receptor binding activities of new N-heteroaromatic 5/6-ring Mannich bases.

Sabine Linz, Jörg Müller, Harald Hübner, Peter Gmeiner, Reinhard Troschütz

Index: Bioorg. Med. Chem. 17 , 4448-58, (2009)

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Abstract

A series of phenylpiperazine-methyl-substituted 1H-pyrrolo[2,3-c]pyridine, imidazo[1,2-c]-, pyrrolo[2,3-d]- and pyrrolo[3,2-d]pyrimidines were prepared as selective dopamine D4-ligands. The pyrrolo[2,3-d]pyrimidine derivatives 12d (K(i)=1,9 nM) and 34 d (K(i)=2,4 nM) as well as the pyrrolo[3,2-d]pyrimidine Mannich base 49f (K(i)=2,8 nM) showed high dopamine D4 receptor activity superior to the atypical antipsychotic agent clozapine.