Quinazolinone novel derivatives synthesis and their Biological Evaluation as Antimicrobial and Antitubercular agents

Abstract

At a global level, tuberculosis (TB) is the disease of human values. It suffers from major health, social and economic burden in many countries. There is an inability of an effective vaccine or the use of vaccine were too long and expensive, have increased risk of spread of this disease. A series of quinazolinone derivatives prepared with the help of 2-Amino-3,4,5-trimethoxy benzoic acid and Vilsmeir reagent. Synthesized compounds were characterized by various spectral methods. Different activity like antimicrobial activity of the synthesised compounds were performed, and the most active compounds of the series were further screened for antitubercular activity against bacteria mycobacterium H37Rv. Results showed that all the synthesized compounds have antimicrobial activity. Compounds IV c, IV f, IV h and IV o showed maximum activity in the synthesized series. These four compounds further screened for antitubercular activity. Compounds IV c, IV f, IV h and IV o showed significant antitubercular activity.

Design and Synthesis of Quinazolinone-Triazole Hybrids as Potent Anti-Tubercular Agents

“…From medicinal chemists’ viewpoint, 2,3-dihydroquinazolin-4­(1 H )-ones have received immense attention in the last few decades as they possess a wide range of biological activities. − Therefore, efforts have been devoted in developing effective, new, and useful synthetic protocols for 2,3-dihydroquinazolin-4­(1 H )-ones. Among the therapeutic activities, large numbers of quinazolines also show anti-tubercular (anti-TB) activity with moderate to excellent potency − (Figure ).…”

Synthesis and antimycobacterial evaluation of pyrazinamide, benzimidazole and carboxamide derivatives

“…TB is highly contagious when the disease is active and can infect the lungs and affect other parts of the body [1]. Robert Koch identified TB in 1882 and since his discovery to till date now, the global TB epidemic looks unchanged [2].…”