Pyrazolo[1,5-a]pyrimidine acetamides: 4-Phenyl alkyl ether derivatives as potent ligands for the 18 kDa translocator protein (TSPO) |
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| Authors: | Aaron Reynolds Raphy Hanani David Hibbs Annelaure Damont Eleonora Da Pozzo Silvia Selleri Frédéric Dollé Claudia Martini Michael Kassiou |
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| Institution: | 1. School of Chemistry, University of Sydney, Sydney, NSW 2006, Australia;2. Faculty of Pharmacy, University of Sydney, Sydney, NSW 2006, Australia;3. CEA, I2BM, Service Hospitalier Frédéric Joliot, F-91401 Orsay, France;4. Department of Psychiatry, Neurobiology, Pharmacology and Biotechnology, University of Pisa, Via Bonanno, 6 56126 Pisa, Italy;5. Department of Pharmaceutical Sciences, University of Florence, Via U. Schiff, 650019 Polo Scientifico Sesto Fiorentino, Italy;6. Brain and Mind Research Institute, Sydney, NSW 2050, Australia;7. Discipline of Medical Radiation Sciences, University of Sydney, Sydney, NSW 2006, Australia |
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| Abstract: | Herein, we report the synthesis of four new phenyl alkyl ether derivatives (7, 9–11) of the pyrazolo1,5-a]pyrimidine acetamide class, all of which showed high binding affinity and selectivity for the TSPO and, in the case of the propyl, propargyl, and butyl ether derivatives, the ability to increase pregnenolone biosynthesis by 80–175% over baseline in rat C6 glioma cells. While these compounds fit our in silico generated pharmacophore for TSPO binding the current model does not account for the observed functional activity. |
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