Li Guca
2014
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Journal
Chinese Journal of Applied Chemistry
Abstract
3-( 4-Benzylpiperazin-1-ylmethyl) pyrazolo[1,5-α]pyridine,3-[4-( 4-chlorobenzyl) piperazin-1-ylmethyl]pyrazolo[1,5-α]pyridine and 3-[4-( 4-methoxybenzyl) piperazin-1-ylmethyl] pyrazolo[1,5-a] pyridine were synthesized from pyrazolo [1,5-α]pyridine-3-carbaldehyde and 1-piperazinearboxaldehyde through reductive amination,amide hydrolysis and N-alkylation. The structures of the intermediates and the target compounds were confirmed by1H NMR and ESI MS. Through in vitro receptor binding assay,the affinity constants( Ki) of the target compounds were determined to be 1. 6,7. 2,65 nmol/L for D4receptor; 1920,5320,9800 nmol / L for D2receptor; 1710,4270 and 5600 nmol / L for dopamine D3receptor, respectively. The results suggested that 3-( 4-benzylpiperazin-1-ylmethyl) pyrazolo[1,5-α] pyridine is a potential dopamine D4receptor ligand.