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Novel 3, 6, 7-substituted pyrazolopyrimidines as positive allosteric modulators for the hydroxycarboxylic acid receptor 2 (GPR109A)

Blad, Clara C; van Veldhoven, Jacobus P D; Klopman, Corné; Wolfram, Dieter R; Brussee, Johannes; Lane, J Robert; Ijzerman, Adriaan P

Authors

Clara C Blad

Jacobus P D van Veldhoven

Corné Klopman

Dieter R Wolfram

Johannes Brussee

J Robert Lane

Adriaan P Ijzerman



Abstract

A number of pyrazolopyrimidines were synthesized and tested for their positive allosteric modulation of the HCA(2) receptor (GPR109A). Compound 24, an efficacious and potent agonist and allosteric enhancer of nicotinic acid's action, was the basis for most other compounds. Interestingly, some of the compounds were found to increase the efficacy of the endogenous ligand 3-hydroxybutyrate and enhance its potency almost 10-fold. This suggests that the pyrazolopyrimidines may have therapeutic value when given alone.

Journal Article Type Article
Publication Date Mar 15, 2012
Journal Journal of Medicinal Chemistry
Print ISSN 0022-2623
Publisher American Chemical Society
Peer Reviewed Peer Reviewed
Volume 55
Issue 7
Pages 3563-3567
APA6 Citation Blad, C. C., van Veldhoven, J. P. D., Klopman, C., Wolfram, D. R., Brussee, J., Lane, J. R., & Ijzerman, A. P. (2012). Novel 3, 6, 7-substituted pyrazolopyrimidines as positive allosteric modulators for the hydroxycarboxylic acid receptor 2 (GPR109A). Journal of Medicinal Chemistry, 55(7), 3563-3567. https://doi.org/10.1021/jm300164q
DOI https://doi.org/10.1021/jm300164q
Publisher URL https://pubs.acs.org/doi/full/10.1021/jm300164q


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