原创力文档discovery of new nanomolar inhibitors of gpa extension of 2-oxo-1,2-dihydropyridinyl-3-yl amide-based gpa inhibitors：（新发现的摩尔抑制剂2-oxo-1的gpa的延伸,2-dihydropyridinyl-3-yl amide-based gpa抑制剂）.pdfVIP
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discovery of new nanomolar inhibitors of gpa extension of 2-oxo-1,2-dihydropyridinyl-3-yl amide-based gpa inhibitors：（新发现的摩尔抑制剂2-oxo-1的gpa的延伸,2-dihydropyridinyl-3-yl amide-based gpa抑制剂）
European Journal of Medicinal Chemistry 127 (2017) 341e356
Contents lists available at ScienceDirect
European Journal of Medicinal Chemistry
journal homepage: /locate/ejmech
Research paper
Discovery of new nanomolar inhibitors of GPa: Extension of 2-oxo-1,2-
dihydropyridinyl-3-yl amide-based GPa inhibitors
Wendy A. Loughlin a, *, Ian D. Jenkins b, N. David Karis b, Peter C. Healy a, c
a School of Natural Sciences, Griffi th University, Brisbane, Qld, 4111, Australia
b Eskitis Institute for Drug Discovery, Griffi th University, Brisbane, Qld, 4111, Australia
c Central Analytical Research Facility, Queensland University of Technology, Brisbane, Qld, 4001, Australia
a r t i c l e i n f o a b s t r a c t
Article history: Glycogen Phosphorylase (GP) is a functionally active dimeric enzyme, which is a target for inhibition of
Received 24 November 2016 the conversion of glycogen to glucose-1-phosphate. In this study we report the design and synthesis of
Received in revised form 14 new pyridone derivatives, and seek to extend the SAR analysis of these compounds. The SAR revealed
22 December 2016
the minor influence of the amide group, importance of the pyridone ring both spatially around the
Accepted 23 December 2016
Available online 26 December 2016 pyridine ring and for possible p-stacking, and confirmed a preference for inclusion of 3,4-dichlorobenzyl
moieties, as bookends to the pyridone scaffold. Upon exploring a dimer strategy as part of the SAR
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