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-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.
journal_name
Chem Biol Drug Desjournal_title
Chemical biology & drug designauthors
Kumari N,Chadha N,Srivastava P,Mishra LC,Bhagat S,Mishra AK,Tiwari AKdoi
10.1111/cbdd.12971subject
Has Abstractpub_date
2017-10-01 00:00:00pages
511-519issue
4eissn
1747-0277issn
1747-0285journal_volume
90pub_type
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