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

Deepakumari, Hemavathi N; Jayanna, Bidarur K; Prashanth, Maralekere K; Revanasiddappa, Hosakere D; Veeresh, Bantal

Deepakumari, Hemavathi N; Jayanna, Bidarur K; Prashanth, Maralekere K; Revanasiddappa, Hosakere D; Veeresh, Bantal.

Afiliación

Deepakumari HN; Department of Chemistry, Bharathi College, Bharathinagara, Mandya, Karnataka, India.
Jayanna BK; Department of Chemistry, B. N. M. Institute of Technology, Bangaluru, Karnataka, India.
Prashanth MK; Department of Chemistry, B. N. M. Institute of Technology, Bangaluru, Karnataka, India.
Revanasiddappa HD; Department of Chemistry, University of Mysore, Manasagangothri Mysore, Karnataka, India.
Veeresh B; Department of Pharmacology, G Pullareddy College of Pharmacy, Mehdipatnam, Hyderabad, India.

Arch Pharm (Weinheim) ; 349(7): 566-71, 2016 Jul.

Article en En | MEDLINE | ID: mdl-27231098

RESUMEN

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.

Asunto(s)

Anticonvulsivantes/síntesis química; Anticonvulsivantes/uso terapéutico; Quinazolinas/síntesis química; Quinazolinas/uso terapéutico; Convulsiones/tratamiento farmacológico; Animales; Relación Dosis-Respuesta a Droga; Electrochoque; Metacualona/uso terapéutico; Ratones; Pentilenotetrazol; Picrotoxina/uso terapéutico; Convulsiones/inducido químicamente; Relación Estructura-Actividad; Ácido Valproico/uso terapéutico

Palabras clave

Anticonvulsant; Glycosmicine; MES; Neurotoxicity; PTZ

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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Quinazolinas / Convulsiones / Anticonvulsivantes Límite: Animals Idioma: En Revista: Arch Pharm (Weinheim) Año: 2016 Tipo del documento: Article País de afiliación: India Pais de publicación: Alemania

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