title: Synthesis and evaluation of 3-anilino-quinoxalinones as glycogen phosphorylase inhibitors.
abstract: A series of 3-anilino-quinoxalinones has been identified as a new class of glycogen phosphorylase inhibitors. The lead compound 1 was identified through high throughput screening as well as through pharmacophore-based electronic screening. Modifications were made to the scaffold of 1 to produce novel analogues, some of which are 25 times more potent than the lead compound.
authors.affiliation: Johnson & Johnson Pharmaceutical Research and Development, L.L.C., 1000 Rt. 202, PO Box 300, Raritan, NJ 08869, USA. jdudash@prdus.jnj.com
authors.forename: Joseph
authors.initials: J
authors.lastname: Dudash
authors.forename: Yongzheng
authors.initials: Y
authors.lastname: Zhang
authors.forename: John B
authors.initials: JB
authors.lastname: Moore
authors.forename: Richard
authors.initials: R
authors.lastname: Look
authors.forename: Yin
authors.initials: Y
authors.lastname: Liang
authors.forename: Mary Pat
authors.initials: MP
authors.lastname: Beavers
authors.forename: Bruce R
authors.initials: BR
authors.lastname: Conway
authors.forename: Philip J
authors.initials: PJ
authors.lastname: Rybczynski
authors.forename: Keith T
authors.initials: KT
authors.lastname: Demarest
mesh_terms: D000818:Animals; D001786:Blood Glucose / Q000187:drug effects; D004353:Drug Evaluation, Preclinical; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000493:pharmacokinetics; D024981:Glycogen Phosphorylase / Q000037:antagonists & inhibitors*; D007004:Hypoglycemic Agents / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D020128:Inhibitory Concentration 50; D051379:Mice; D008820:Mice, Obese; D011810:Quinoxalines; D013329:Structure-Activity Relationship
chemical_list: D001786:Blood Glucose; D004791:Enzyme Inhibitors; D007004:Hypoglycemic Agents; D011810:Quinoxalines; D024981:Glycogen Phosphorylase