Novel indolizine compounds as potent inhibitors of phosphodiesterase IV (PDE4): Structure-activity relationship
摘要：
A series of novel indolizine 2-oxoacetamides were designed and synthesized as PDE4 inhibitors. Preliminary SAR of this new class of compounds revealed key structural features required for high potency. Compounds1aband2aare among the most potent inhibitors of PDE4 with low single nM IC50. Cellular activity was demonstrated by the inhibition of TNFα production from human PBMC with IC50ranging from 14 to 72 nM. Docking analyses suggest the OH group in1abenhance the bindingviaan H-bond interaction with the PDE4 enzyme.
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关键词：
cyanobacteria Anabaena circinalis paralytic shellfish toxin saxitoxin chemical derivatization standard
DOI：
10.1039/C0MD00215A
被引量：
年份：
2011
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