N-(4-(4-(2, 3-Dichloro-or 2-methoxyphenyl) piperazin-1-yl) butyl) heterobiarylcarboxamides with Functionalized Linking Chains as High Affinity and Enantioselective …
…, JR Deschamps, M Taylor, R Kumar, D Ho…
文献索引：Newman, Amy Hauck; Grundt, Peter; Cyriac, George; Deschamps, Jeffrey R.; Taylor, Michelle; Kumar, Rakesh; Ho, David; Luedtke, Robert R. Journal of Medicinal Chemistry, 2009 , vol. 52, # 8 p. 2559 - 2570
In the present report, the D3 receptor pharmacophore is modified in the 2, 3-diCl-and 2- OCH3-phenylpiperazine class of compounds with the goal to improve D3 receptor affinity and selectivity. This extension of structure− activity relationships (SAR) has resulted in the identification of the first enantioselective D3 antagonists (R-and S-22) to be reported, wherein enantioselectivity is more pronounced at D3 than at D2, and that a binding region ...
