Design and synthesis of quinazolinone derivatives as a novel antitubercular agents

[摘要] Quinazolinone is a compound made up of two fused six member simple aromatic rings-benezene and pyrimidine ring and have been reported to posses versatile type of biological activities such as anticancer, anticonvulsant, antiinflammatory, antihelminthic, antimicrobial activities. A series of novel substituted- [1,2,4]triazolo[1,5c]quinazolinone derivatives (K11-19) were synthesized by mannich reaction using formamide and different secondary amines. Structures of compounds synthesized were confirmed by IR, 1H-NMR and Mass spectroscopic analysis. All synthesized compounds were screened for anti-tubercular activity. The anti-tubercular activity of synthesized compounds was performed against M. tuberculosis H37Rv at concentration 30 μg/ml using Streptomycin and Pyrazinamide 7.5 μg/ml as standard drug. All synthesized compounds have shown anti-tubercular activity as compared to standard drug Streptomycin, Pyrazinamide. Compounds K 13 and K 17 have shown very good anti-tubercular activity.

[学科分类] 药理学