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A prior study reported on hydroxy substituted 2-benzylidene-1-indanone derivatives as A and/or A antagonists for the potential treatment of neurological conditions. A lead compound () was identified with both A and A affinity in the micromolar range. The current study explored the structurally related methoxy substituted 2-benzylidene-1-indanone derivatives with various substitutions on ring A and B of the benzylidene indanone scaffold in order to enhance A and A affinity. This led to compounds with both A and A affinity in the nanomolar range, namely (A (rat) = 41 nM; A (rat) = 97 nM) with C4-OCH substitution on ring A together with (3') hydroxy substitution on ring B and (A (rat) = 42 nM; A (rat) = 78 nM) with C4-OCH substitution on ring A together with (3') and (4') dihydroxy substitution on ring B. Additionally, is an A antagonist. Consequently, the methoxy substituted 2-benzylidene-1-indanone scaffold is highly promising for the design of novel A and A antagonists.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6390816 | PMC |
| http://dx.doi.org/10.1039/c8md00540k | DOI Listing |
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