Pyrido pyrimidinones as selective agonists of the high affinity niacin receptor GPR109A: optimization of in vitro activity

…, H Kühne, H Dehmlow, U Grether, A Conte…

Index: Peters, Jens-Uwe; Kuehne, Holger; Dehmlow, Henrietta; Grether, Uwe; Conte, Aurelia; Hainzl, Dominik; Hertel, Cornelia; Kratochwil, Nicole A.; Otteneder, Michael; Narquizian, Robert; Panousis, Constantinos G.; Ricklin, Fabienne; Roever, Stephan Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 18 p. 5426 - 5430

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Citation Number: 10

Abstract

Pyrido pyrimidinones are selective agonists of the human high affinity niacin receptor GPR109A (HM74A). They show no activity on the highly homologous low affinity receptor GPR109B (HM74). Starting from a high throughput screening hit the in vitro activity of the pyrido pyrimidinones was significantly improved providing lead compounds suitable for further optimization.