4 years ago

Modified benzoxazolone derivative as 18-kDa TSPO ligand

Modified benzoxazolone derivative as 18-kDa TSPO ligand
Anjani K. Tiwari, Anil K. Mishra, Nidhi Chadha, Lokesh Chandra Mishra, Sunita Bhagat, Pooja Srivastava, Neelam Kumari
We have synthesized six new congeners of acetamidobenzoxazolone for Translocator Protein [18 kDa, TSPO] imaging. The best in vitro binding affinity (10.8 ± 1.2 nm) for TSPO was found for N-methyl-2-(5-(naphthalen-1-yl)-2-oxobenzo[d]oxazol-3(2H)-yl)-N-phenylacetamide, (NBMP). NBMP was synthesised by Suzuki coupling reaction between 2-(5-bromo-2-oxo-1,3-benzoxazol-3(2H)-yl)-N-phenylacetamide and napthalene-1-boronic acid. Computational docking and simulation studies showed not much impact of intersubject variability on binding which is one of the major drawbacks of several TSPO ligands. These findings suggested that NBMP may become a promising marker for visualization of neuroinflammation via TSPO targeting. A new congener of acetamidobenzoxazolone called as NBMP or 2-[5 (naphthyl)amino-2-oxobenzo-2-oxo-1,3-benzoxazol-3(2H)-yl]-N-methyl-N-penylacetamide has shown 10.8 ± 1.2 nm binding affinity towards TSPO under in vitro conditions.

Publisher URL: http://onlinelibrary.wiley.com/resolve/doi

DOI: 10.1111/cbdd.12971

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