Modified benzoxazolone derivative as 18- kDa TSPO ligand.

Autor:	Kumari, Neelam, Chadha, Nidhi, Srivastava, Pooja, Mishra, Lokesh Chandra, Bhagat, Sunita, Mishra, Anil K., Tiwari, Anjani K.
Předmět:	TRANSLOCATOR proteins LIGANDS (Biochemistry) CHEMICAL synthesis IN vitro studies INFLAMMATION
Zdroj:	Chemical Biology & Drug Design; Oct2017, Vol. 90 Issue 4, p511-519, 10p
Abstrakt:	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 n m) for TSPO was found for N-methyl-2-(5-(naphthalen-1-yl)-2-oxobenzo[ d]oxazol-3(2 H)-yl)- N-phenylacetamide, ( NBMP). NBMP was synthesised by Suzuki coupling reaction between 2-(5-bromo-2-oxo-1,3-benzoxazol-3(2 H)-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. [ABSTRACT FROM AUTHOR]
Databáze:	Complementary Index
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