Halogenated benzofuran compounds show selective MAO-B inhibition in lab tests
Researchers synthesized ten halogenated benzofuran derivatives and tested their ability to inhibit monoamine oxidase enzymes. One compound, BF2, demonstrated the strongest and most selective MAO-B inhibition with a reversible mechanism.
link.springer.comTen halogenated benzofuran derivatives labeled BF1 through BF10 were synthesized and tested for activity against monoamine oxidase A and B enzymes. All ten compounds inhibited MAO-B more strongly than MAO-A. BF2 recorded the lowest IC₅₀ value at 0.082 µM, followed by BF5 at 0.095 µM and BF1 at 0.16 µM.
Selectivity and mechanism BF2 showed a selectivity index of 1038.05 for MAO-B over MAO-A. Kinetic analysis indicated competitive inhibition with a Ki value of 0.083 ± 0.0056 µM. Dialysis experiments confirmed that BF2 inhibition is reversible, matching the profile of the reference compound safinamide.
BF5 showed no cytotoxicity in L929 cell assays. Both compounds displayed moderate blood-brain barrier permeability in PAMPA testing. Molecular docking studies indicated that BF2 interacts with MAO-B through π–π stacking with residues Tyr326 and Tyr398.
Molecular dynamics simulations supported stable binding of BF2 in the MAO-B active site. The work was funded in part by the Deanship of Research and Graduate Studies at King Khalid University under grant RGP2/330/47.
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