The aim of the present study was to evaluate the anticonvulsant effects of alcoholic root extract of Cardiospermum halicacabum L., Sapindaceae (ARECH), on the various murine models of epilepsy. The root extract of the plant was administered p.o. to male swiss albino mice at doses of 30, 100 and 300 mg/kg before evaluation. The brain monoamine levels were determined after two days administration. ARECH at doses of 100 and 300 mg/kg significantly delayed the onset of clonus and tonus in pentylenetetrazol, isoniazid and picrotoxin-induced convulsions. Tonic hind limb extension was also decreased at doses of 100 and 300 mg/kg as compared to vehicle control in maximal electroshock model. No significant motor toxicity was observed even at a highest dose administered, i.e. 900 mg/kg. Brain monoamine analysis by HPLC revealed a significant increase in GABAergic activity in C+ (in cerebellum) and C- (except cerebellum). These results suggested that ARECH possesses a significant anticonvulsant activity with a low motor toxicity profile. This activity may be attributed to an increase in GABAergic activity.

Uma estratégia conveniente em três etapas é proposta para a síntese de mono e bis-indolo[1,2-c] quinazolinas, a partir de 2-(2-aminofenil)indol e aril aldeídos. Os novos compostos sintetizados foram caracterizados por análise elementar, IV, ¹H RMN, 13C RMN, e espectrometria de massa. Todos os derivados foram testados para avaliação das suas atividades antibacterial (S. aureus, B. subtilis, S. pyogenes, S. typhimurium, E. coli, K. pneumonia) e antifúngica (A. niger, C. albicans, T. viridae) usando o método cup plate. Dentre os compostos testados, as mono- indolo[1,2-c] quinazolinas (15-18) exibiram boas atividades antibacteriais, enquanto 15 e 18 também mostraram notável atividade antifúngica. Especialmente, 19 e 20 exibiram forte atividade antibacteriana e antifúngica contra todas as cepas testadas.

A convenient three-step strategy is proposed for the synthesis of mono and bis-indolo[1,2-c] quinazolines from 2-(2-aminophenyl)indole and various aryl aldehydes. The newly synthesized compounds were characterized by elemental analysis, IR, ¹H NMR, 13C NMR, and mass spectroscopic investigation. All the derivatives were screened for antibacterial (S. aureus, B. subtilis, S. pyogenes, S. typhimurium, E. coli, K. pneumonia) and antifungal (A. niger, C. albicans, T. viridae) activities by cup plate method. Among the compounds tested, mono- indolo[1,2-c] quinazolines (15-18) exhibited good antibacterial activities while 15 and 18 also showed notable antifungal activity. Especially, 19 and 20 exhibited stronger antibacterial as well as antifungal activity against all tested strains.

Uma série de compostos 6-arilbenzimidazo[1,2-c]quinazolina (11-20) foram sintetizados pela condensação do 2-(o-aminofenil)benzimidazol com diferentes arilaldeídos seguida pela ciclização oxidativa dos 2-o-arilidenoaminofenilbenzimidazol (1-10). Todos os produtos foram caracterizados por espectroscopia no infravermelho (IR), ressonância magnética nuclear de prótons e de carbono, (RMN ¹H e RNN 13C), de massas (MS) e análise elementar. A atividade antimicrobial de todos os 6-arilbenzimidazo[1,2-c]quinazolina foi testada com três linhagens de bactérias Gram-positivas (S. aureus, B. subtilis e S. pyogenes), três Gram-negativas (S. typhimurium, E. coli e K. pneumonia) e de três linhagens de fungos (A. niger, C. albicans e T. viridae). Dos compostos testados, o 13, o 19 e o 20 mostraram-se ser os mais potentes inibidores contra os organismos testados.

A series of 6-arylbenzimidazo[1,2-c]quinazoline compounds (11-20) were synthesised by the condensation of 2-(o-aminophenyl)benzimidazole with different arylaldehydes, followed by oxidative cyclisation of the resulting 2-o-arylideneaminophenylbenzimidazoles (1-10). All the products were characterized via IR, ¹H NMR, 13C NMR, MS and elemental analysis. The antimicrobial activities of all 6-arylbenzimidazo [1,2-c]quinazolines against three Gram-positive (S. aureus, B. subtilis, S. pyogenes), three Gram-negative (S. typhimurium, E. coli, K. pneumonia) bacteria and three fungal strains (A. niger, C. albicans, T. viridae) were evaluated. Among the compounds tested 13, 19 and 20 showed most potent inhibitory action against test organisms.