Synthesis and Anticonvulsant Activity of N‐(Substituted)‐1‐methyl‐2,4‐dioxo‐1,2‐dihydroquinazoline‐3(4H)‐carboxamides

Abstract

A series of new N-(substituted)-1-methyl-2,4-dioxo-1,2-dihydroquinazoline-3(4H)-carboxamides were designed, synthesized, and evaluated for their anticonvulsant activity. Most of the synthesized compounds exhibited potent anticonvulsant activities in the maximal electroshock (MES) and pentylenetetrazol (PTZ) test. The most promising compound 4c showed significant anticonvulsant activity with a protective index value of 3.58. The compounds 4a-c were also found to have encouraging anticonvulsant activity in the MES and PTZ screen when compared with the standard drugs, valproate and methaqualone. The same compounds were found to exhibit advanced anticonvulsant activity as well as lower neurotoxicity than the reference drugs.

Synthesis and Evaluation of 5‐(o‐Tolyl)‐1H‐tetrazole Derivatives as Potent Anticonvulsant Agents

“…The anticonvulsant activity of the synthesized compounds ( 3a – j ) was determined using two animal models of seizure according to the standard protocols within the Antiepileptic Drug Development (ADD) Program at National Institute of Neurological Disorders and Stroke, National Institutes of Health, Rockville, USA which included maximal electroshock seizure (MES) and subcutaneous pentylenetetrazole (scPTZ) . Almost all clinically significant AEDs are protective in at least one of these two models . In addition to the initial anticonvulsant screen, acute neurotoxocity (NT) was evaluated in the rotarod test .…”

Quinazoline pharmacophore in therapeutic medicine

“…carboxamides unveiled them to possess improved and better anticonvulsant activity when compared with clinical standard drugs which are valproate and methaqualone (Deepakumari et al, 2016). Methaqualone 15 as a quinazoline analog is an important landmark in the field of synthetic anticonvulsants (Kashaw et al, 2009).…”

Design, synthesis, anticancer activity and docking studies of novel quinazoline-based thiazole derivatives as EGFR kinase inhibitors

“…The most significant categories of heterocyclic chemicals in terms of pharmacology are quinazolines [ 12 ]. Due to the quinazolinone nucleus' stability, medicinal chemists have been motivated to add a variety of bioactive moieties to create novel potential therapeutic medicines [ [13] , [14] , [15] , [16] ]. Due to its wide range of biological activity, the quinazolinone skeleton is a commonly encountered heterocycle in the drug development process [ 17 ].…”