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Abstract
Benzothiazoloquinazolines are known to possess several interesting biological properties. Various arylated benzothiazoloquinazolines were synthesized from readily available 2
‐
bromo
‐
12
H
‐
benzothiazolo[2,3
‐
b
]quinazolin
‐
12
‐
one by palladium catalysed Suzuki
‐
Miyaura reactions in 43 – 85% yield. Synthesized derivatives were analysed regarding their
in vitro
inhibition activity towards monoamine oxidases A and B and showed significant inhibitory values in the micromolar range. Molecular modelling as well as PAINS studies on the binding interaction of most potent inhibitors with both isoforms were studied to verify the experimental results.