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

Full Text: HTML

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.

Related Articles:

Copper (ii)-catalyzed C–O coupling of aryl bromides with aliphatic diols: synthesis of ethers, phenols, and benzo-fused cyclic ethers

[Liu, Yajun; Park, Se Kyung; Xiao, Yan; Chae, Junghyun Organic and Biomolecular Chemistry, 2014 , vol. 12, # 26 p. 4747 - 4753]

The gas??phase Smiles rearrangement the effect of ring substitution. An 18O labelling study

[Eichinger, Peter C. H.; Bowie, John H. Organic Mass Spectrometry, 1992 , vol. 27, # 10 p. 995 - 999]

More Articles...