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Synthesis and Characterization of Selective Dopamine D2 Receptor Antagonists. 2. Azaindole, Benzofuran, and Benzothiophene Analogs of L-741,626

Synthesis and Characterization of Selective Dopamine D2 Receptor Antagonists. 2. Azaindole, Benzofuran, and Benzothiophene Analogs of L-741,626

Suwanna Vangveravong, Michelle Taylor, Jinbin Xu, Jinquan Cui, Wesley Calvin, Sonja Babic, Robert R Luedtke, Robert H Mach

Bioorg Med Chem. 2010 Jul 15;18(14):5291-300.

PMID: 20542439

Abstract:

A series of indole, 7-azaindole, benzofuran, and benzothiophene compounds have been prepared and evaluated for affinity at D2-like dopamine receptors. These compounds share structural elements with the classical D2-like dopamine receptor antagonists haloperidol, N-methylspiperone and benperidol. Two new compounds, 4-(4-iodophenyl)-1-((4-methoxy-1H-indol-3-yl)methyl)piperidin-4-ol (6) and 4-(4-iodophenyl)-1-((5-methoxy-1H-indol-3-yl)methyl)piperidin-4-ol (7), were found to have high affinity to and selectivity for D2 versus D3 receptors. Changing the aromatic ring system from an indole to other heteroaromatic ring systems reduced the D2 binding affinity and the D2 versus D3 selectivity.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP81226600	L-741,626		81226-60-0	Price

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