Antitubercular and Anticonvulsant Activities of Phenyl-di-hydropyridazinone Derivatives Containing 2-Substituted amin-1-yl-methyl and 2-(2-1H-amin-1-yl) ethyl Moieties

Abstract

Two series of 6-phenyl-4,5-dihydropyridazinone derivatives containing 2-substituted amin-1-yl-methyl (4a-g) and 2-substituted amin-1-yl-ethyl (5a-g) were synthesized and tested as antitubercular and anticonvulsant agents. and in vivo anticonvulsant activities were tested against maximum electroshock (MES) and Isoniazid (INH) induced convulsion methods in male Swiss albino mice. All the compounds (4a- g & 5a-g) were exhibited significant anticonvulsant activities against both MES and INH induced convulsions and compared with phenytoin sodium (25 mg/kg) and sodium vaproate (50 mg/kg) as reference drugs. The compounds (4a-g and 5a-g) were also exhibited anti-tubercular activity, the minimum inhibitory concentration (MIC) of compound 4a (3.12 μg/ml), 4g (6.25 μg/ml) and 4e (0. 2 μg/ml) which were found higher or equal MIC value than reference drugs streptomycin (6.25 μg/ml), pyrizinamide (3.125 μg/ml) and Isoniazid (3.125μg/ml). Other remaining compounds were also exhibited less antitubercular activity than reference drugs. All the compounds (4a-g & 5a-g) were exhibited significant anticonvulsant activities against both MES and INH induced convulsions and also exhibited significant antitubercular activity.