title: 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.
authors.affiliation: Department of Chemistry, Bharathi College, Bharathinagara, Mandya, Karnataka, India.
authors.forename: Hemavathi N
authors.initials: HN
authors.lastname: Deepakumari
authors.affiliation: Department of Chemistry, B. N. M. Institute of Technology, Bangaluru, Karnataka, India.
authors.forename: Bidarur K
authors.initials: BK
authors.lastname: Jayanna
authors.affiliation: Department of Chemistry, B. N. M. Institute of Technology, Bangaluru, Karnataka, India.
authors.forename: Maralekere K
authors.initials: MK
authors.lastname: Prashanth
authors.affiliation: Department of Chemistry, University of Mysore, Manasagangothri Mysore, Karnataka, India.
authors.forename: Hosakere D
authors.initials: HD
authors.lastname: Revanasiddappa
authors.affiliation: Department of Pharmacology, G Pullareddy College of Pharmacy, Mehdipatnam, Hyderabad, India.
authors.forename: Bantal
authors.initials: B
authors.lastname: Veeresh
mesh_terms: D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis* / Q000627:therapeutic use*; D004305:Dose-Response Relationship, Drug; D004597:Electroshock; D008702:Methaqualone / Q000627:therapeutic use; D051379:Mice; D010433:Pentylenetetrazole; D010852:Picrotoxin / Q000627:therapeutic use; D011799:Quinazolines / Q000138:chemical synthesis* / Q000627:therapeutic use*; D012640:Seizures / Q000139:chemically induced / Q000188:drug therapy*; D013329:Structure-Activity Relationship; D014635:Valproic Acid / Q000627:therapeutic use
chemical_list: D000927:Anticonvulsants; D008702:Methaqualone; D010433:Pentylenetetrazole; D010852:Picrotoxin; D011799:Quinazolines; D014635:Valproic Acid
keywords: Anticonvulsant; Glycosmicine; MES; Neurotoxicity; PTZ