No abstract

Several 2‐aryl substituted thiosemicarbazido‐4‐methyl‐6‐methoxyquinolines and 2‐aryl substituted semi‐carbazido 4‐methyl‐6‐methoxyquinolines were synthesized and evaluated for their antimalarial activity in mice infected with Plasmodium berghei. Two of these substituted quinolines were found to exhibit 50% clearance in a dose of 500 mg./kg. administered intraperitoneally for 5 days.

Nine 1-(3,4-dimethoxyphenylethyl)-2-methyl-4-(substituted benzylidene)-5-imidazolones were synthesized, characterized by their sharp melting points, elemental analyses and infrared spectra and evaluated for anticonvulsant activity. All l,2,4-trisubstituted-5-imidazolones at a dose of 100 mg/kg i.p. possessed anticonvulsant activity and the degree of protection observed against pentylenetetrazol-induced convulsions in mice ranged from 20 to 60%. These 1,2,4-trisubstituted-5-imidazolones selectively inhibited in vitro oxidation of the nicotinamide adenine dinucleotide (NAD)-dependent oxidation of pyruvate, α-ketoglutarate and NADH by rat brain homogenates while the NAD-independent oxidation of succinate remained unaltered. The anticonvulsant activity possessed by 1,2,4-trisubstituted-5-imidazolones was unrelated with their ability to selectively inhibit respiratory activity of rat brain homogenates.