Journal
ROYAL SOCIETY OPEN SCIENCE
Volume 7, Issue 4, Pages -Publisher
ROYAL SOC
DOI: 10.1098/rsos.200050
Keywords
monoamine oxidase inhibitors; antidepressant; quinazoline analogues; structure-activity relationships
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Funding
- Deanship of Scientific Research at Taibah University, Al-Madinah Al-Munawarah, Saudi Arabia [7101]
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A new series of N'-substituted benzylidene-2-(4-oxo-2-phenyl-1,4-dihydroquinazolin-3(2H)-ypacetohydrazide (5a-5h) has been synthesized, characterized by FT-IR, NMR spectroscopy and mass spectrometry and tested against human monoamine oxidase (MAO) A and B. Only (4-hyclroxy-3-methoxybenzylidene) substituted compounds gave submicromolar inhibition of MAO-A and MAO-B. Changing the phenyl substituent to methyl on the unsaturated quinazoline ring (12a-12d) decreased inhibition, but a less flexible linker (14a-14d) resulted in selective micromolar inhibition of hMAO-B providing insight for ongoing design. [GRAPHICS] .
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