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

…, J Müller, H Hübner, P Gmeiner, R Troschütz

Index: Linz, Sabine; Mueller, Joerg; Huebner, Harald; Gmeiner, Peter; Troschuetz, Reinhard Bioorganic and Medicinal Chemistry, 2009 , vol. 17, # 13 p. 4448 - 4458

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Citation Number: 18

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 (Ki= 1, 9nM) and 34d (Ki= 2, 4nM) as well as the pyrrolo [3, 2-d] pyrimidine Mannich base 49f (Ki= 2, 8nM) showed high dopamine D4 receptor activity superior to the atypical antipsychotic agent clozapine.