Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 20, Issue 19, Pages 5799-5802Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.07.135
Keywords
Peripheral-type benzodiazepine receptor; Translocator protein; TSPO; Steroidogenesis; Pyrazolo[1,5-a]pyrimidine; Neurodegeneration; Neuroprotection; Microglia
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Funding
- National Institute of Mental Health (NIMH PDSP) [NO1MH32004]
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Herein, we report the synthesis of four new phenyl alkyl ether derivatives (7, 9-11) of the pyrazolo[1,5-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. (C) 2010 Elsevier Ltd. All rights reserved.
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