All the newly synthesized compounds had significant anticonvulsant activity. The same two compounds 5a and 5d showed promising activity, while the other compounds have moderate activity. The proposed work is to effort towards the development and identification of novel molecules as anticonvulsant agents by the synthesis of some novel quinazolinone derivatives with improved biological activity.

This study may be useful in the designing of more potent substituted acetamide derivatives as specific MAOA inhibitors.

Background: Chroman-4-one, also known as 2,3-dihydro-1-benzopyran-4-one, is a heterocyclic compound with a benzene nucleus fused to a 2,3-dihydro-g-pyranone ring. The synthesis of chroman-4-one derivatives is a very appealing aspect in the field of natural and medicinal chemistry. Materials and Methods: The (Z)-3-ethylidene-5,7-dimethylthiochroman-4-one derivatives were, synthesized and evaluated intended for their Monoamine oxidases (MAO)-A and MAO-B inhibitory activity using in vitro fluorometric technique. The majority of synthetic process to acquire(Z)-3-ethylidene-5,7-dimethylthiochroman-4-one derivatives engage condensation catalyzed by acid or base of a range of derivatives of 5,7-dimethylchroman-4-one and 4,6-dimethylbenzofuran-3(2H)-one with the benzaldehyde. The Z-isomers that resulted were usually obtained by photoisomerization of the synthesized E-isomers. Synthesized molecules structures (S-1 to S-18) were established by IR, NMR, mass and elemental analysis. Results: The in vitro activity of synthesized (Z)-3-ethylidene-5,7dimethylthiochroman-4-one derivatives against MAO isoform displayed selectivity in the direction of MAO B isoform. The synthesized derivatives S11 of (Z)-3-ethylidene-5,7-dimethylthiochroman-4-one displayed 7.32 µM (IC 50 ) against MAO-B. Conclusion: Weak to moderate electron pumping and withdrawing groups favor selectivity for hMAO-B, whereas strong deactivators render them non-selective for isoforms. Mono-substitution of methoxy groups at the o-and m-positions improves potency while bi-substitution improves potency and selectivity. The active compounds' ADME predictions revealed that these synthesized compounds may possess drug likeliness confirmed by excellent pharmacokinetic profiles.

Two chalcones (4a, 4b) and nine Schiff bases (4c – 4k) of 7-hydroxy-3-formyl chromen-4-one have been synthesized. All the synthesized compounds 1–18 were screened for their hMAO (human Mono Amine Oxidase) inhibitory activity using recombinant human MAO isoforms. hMAO inhibitory activity was determined by measuring the production of H2O2 from p-tyramine, the common substrate for both hMAO-A and hMAO-B, using the Amplex1-RedMAO assay kit. The compounds and reference inhibitors did not react directly with the Amplex1-Red reagent indicating that they do not interfere with the measurements. The compounds were also confirmed, as they did not interact with resorufin by treating the maximum concentration of compounds with various concentrations of resorufin in order to detect if the fluorescence signal is the same with or without our compounds in the medium. No significant quenching of resorufin was observed.