Synthesis, Molecular Docking and Evaluation of 3-{4-[2-amino-4-(substitutedphenyl)-2H-[1, 3] oxazin/thiazin-6-yl} 2-phenyl-3H-quinazolin-4-one Derivatives for their Anticonvulsant Activity

Abstract

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.

Synthesis and evaluation of anticancer, antiphospholipases, antiproteases, and antimetabolic syndrome activities of some 3H-quinazolin-4-one derivatives

“…In addition to this, many marketed drugs or experimental drug candidates incorporate this pharmacophore as part of the overall topography of the molecules 16 such as ispinesib, nolatrexed, and raltitrexed (the anticancer agents); afloqualone with sedative and muscle relaxant effects, balaglitazone with antidiabetic activities, proquazone (as non-steroidal anti-inflammatory agent), and elinogrel (as reversible P2Y12 receptor antagonist) which is used for the treatment of acute coronary syndrome. Moreover, several new methodologies have been developed for the synthesis of 4-quinazolinone derivatives either using one pot multicomponent approaches 17 or via multistep routes for investigating their pharmacological potential as dual EGFR/HER2 inhibitors 18 , phosphoinositide 3-kinase inhibitors 19 , and as antihypertensive 20 , antioxidant 21 , anticonvulsant 22 , and anti-inflammatory 23 agents.…”

Reverse vaccinology and subtractive genomics approaches for identifying common therapeutics against Mycobacterium leprae and Mycobacterium lepromatosis

“…MHOLline utilizes multi-fasta file of amino acids as an input data for model generation using the MODELLER program. The adopted methodology was revised accordingly from the original work published earlier [21,24,[34][35][36]. The final identified candidate drug targets were prioritized based on criteria (i) the target must have no homology with host; (ii) the target must be a core gene of the pathogen; (iii) the target involved in the pathogen's unique pathway or multiple pathways are considered superior; (iv) pathways with multiple targets are superior to those having just a single target; (v) in the case of enzyme, targets in hostpathogen common pathways, should not be of the same class of protein, and the EC.…”