Tags

Type your tag names separated by a space and hit enter

Pyrido pyrimidinones as selective agonists of the high affinity niacin receptor GPR109A: optimization of in vitro activity.
Bioorg Med Chem Lett. 2010 Sep 15; 20(18):5426-30.BM

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.

Authors+Show Affiliations

Pharma Research, F. Hoffmann-La Roche Ltd, 4070 Basel, Switzerland.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article

Language

eng

PubMed ID

20724150

Citation

Peters, Jens-Uwe, et al. "Pyrido Pyrimidinones as Selective Agonists of the High Affinity Niacin Receptor GPR109A: Optimization of in Vitro Activity." Bioorganic & Medicinal Chemistry Letters, vol. 20, no. 18, 2010, pp. 5426-30.
Peters JU, Kühne H, Dehmlow H, et al. Pyrido pyrimidinones as selective agonists of the high affinity niacin receptor GPR109A: optimization of in vitro activity. Bioorg Med Chem Lett. 2010;20(18):5426-30.
Peters, J. U., Kühne, H., Dehmlow, H., Grether, U., Conte, A., Hainzl, D., Hertel, C., Kratochwil, N. A., Otteneder, M., Narquizian, R., Panousis, C. G., Ricklin, F., & Röver, S. (2010). Pyrido pyrimidinones as selective agonists of the high affinity niacin receptor GPR109A: optimization of in vitro activity. Bioorganic & Medicinal Chemistry Letters, 20(18), 5426-30. https://doi.org/10.1016/j.bmcl.2010.07.108
Peters JU, et al. Pyrido Pyrimidinones as Selective Agonists of the High Affinity Niacin Receptor GPR109A: Optimization of in Vitro Activity. Bioorg Med Chem Lett. 2010 Sep 15;20(18):5426-30. PubMed PMID: 20724150.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Pyrido pyrimidinones as selective agonists of the high affinity niacin receptor GPR109A: optimization of in vitro activity. AU - Peters,Jens-Uwe, AU - Kühne,Holger, AU - Dehmlow,Henrietta, AU - Grether,Uwe, AU - Conte,Aurelia, AU - Hainzl,Dominik, AU - Hertel,Cornelia, AU - Kratochwil,Nicole A, AU - Otteneder,Michael, AU - Narquizian,Robert, AU - Panousis,Constantinos G, AU - Ricklin,Fabienne, AU - Röver,Stephan, Y1 - 2010/07/29/ PY - 2010/06/17/received PY - 2010/07/23/revised PY - 2010/07/25/accepted PY - 2010/8/21/entrez PY - 2010/8/21/pubmed PY - 2010/12/29/medline SP - 5426 EP - 30 JF - Bioorganic & medicinal chemistry letters JO - Bioorg Med Chem Lett VL - 20 IS - 18 N2 - 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. SN - 1464-3405 UR - https://www.unboundmedicine.com/medline/citation/20724150/Pyrido_pyrimidinones_as_selective_agonists_of_the_high_affinity_niacin_receptor_GPR109A:_optimization_of_in_vitro_activity_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0960-894X(10)01077-2 DB - PRIME DP - Unbound Medicine ER -