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Modified benzoxazolone derivative as 18‐kDa TSPO ligand |
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| Authors: | Neelam Kumari Nidhi Chadha Pooja Srivastava Lokesh Chandra Mishra Sunita Bhagat Anil K Mishra Anjani K Tiwari |
| Institution: | 1. Division of Cyclotron and Radiopharmaceutical Sciences (DCRS), Institute of Nuclear Medicine and Allied Sciences (INMAS), DRDO, New Delhi, India;2. Organic Synthesis Research Laboratory, Department of Chemistry, A.R.S.D.College, University of Delhi, University of Delhi, New Delhi, India;3. Department of Biological Sciences, Hans Raj College, North Campus, University of Delhi, New Delhi, India |
| Abstract: | 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‐oxobenzod]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. |
| Keywords: | benzoxazolone microglia activation neuroinflammation translocator protein (18kDa TSPO) |