新型苯并咪唑-吡唑并[1,5-c]喹唑啉类化合物的合成及构效关系研究作为有效的磷酸二酯酶 10A 抑制剂。
Synthesis and SAR study of new phenylimidazole-pyrazolo[1,5-c]quinazolines as potent phosphodiesterase 10A inhibitors.
机构信息
Dipartimento Farmaco Chimico Tossicologico, Università di Sassari, Via F. Muroni 23/a, 07100 Sassari, Italy.
出版信息
Bioorg Med Chem. 2011 Jan 1;19(1):642-9. doi: 10.1016/j.bmc.2010.10.038. Epub 2010 Nov 17.
PMID:21087867
Abstract
A series of phenylimidazole-pyrazolo[1,5-c]quinazolines 1a-q was designed, synthesized and characterised as a novel class of potent phophodiesterase 10A (PDE10A) inhibitors. In this series, 2,9-dimethyl-5-(2-(1-methyl-4-phenyl-1H-imidazol-2-yl)ethyl)pyrazolo[1,5-c]quinazoline (1q) showed the highest affinity for PDE10A enzyme (IC(50)=16nM).
摘要
设计、合成并表征了一系列苯并咪唑-吡唑并[1,5-c]喹唑啉类 1a-q，作为新型强效磷酸二酯酶 10A（PDE10A）抑制剂。在这一系列中，2,9-二甲基-5-(2-(1-甲基-4-苯基-1H-咪唑-2-基)乙基)吡唑并[1,5-c]喹唑啉（1q）对 PDE10A 酶表现出最高的亲和力（IC50=16nM）。
Zotero 插件