Design,synthesis and dopamine D4 receptor binding activities of new N-heteroaromatic 5/6-ring Mannich bases |
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Authors: | Sabine Linz Jörg Müller Harald Hübner Peter Gmeiner Reinhard Troschütz |
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Institution: | Department Chemie und Pharmazie, Lehrstuhl Pharmazeutische Chemie, Friedrich-Alexander-Universität, Schuhstrasse 19, D-91052 Erlangen, Germany |
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Abstract: | A series of phenylpiperazine-methyl-substituted 1H-pyrrolo2,3-c]pyridine, imidazo1,2-c]-, pyrrolo2,3-d]- and pyrrolo3,2-d]pyrimidines were prepared as selective dopamine D4-ligands. The pyrrolo2,3-d]pyrimidine derivatives 12d (Ki = 1,9 nM) and 34d (Ki = 2,4 nM) as well as the pyrrolo3,2-d]pyrimidine Mannich base 49f (Ki = 2,8 nM) showed high dopamine D4 receptor activity superior to the atypical antipsychotic agent clozapine. |
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