International Journal of Pharmaceutical Investigation, 2022, 12, 4, 444-448.
DOI: 10.5530/ijpi.2022.4.76
Published: October 2022
Type: Original Article
Authors:
N Raghavendra Babu
[1]Department of Pharmacy, Koneru Lakshmaiah Education Foundation, Vaddeswaram, Andhra Pradesh, INDIA.[2] Department of Pharmaceutical Chemistry, G. Pulla Reddy Pharmacy, Mehdipatnam, Hyderabad, Telangana, INDIA.
R Subhakar Raju
Department of Pharmacy, Koneru Lakshmaiah Education Foundation, Vaddeswaram, Andhra Pradesh, INDIA.
Narender Malothu
Department of Pharmacy, Koneru Lakshmaiah Education Foundation, Vaddeswaram, Andhra Pradesh, INDIA.
Yenumula Padmavathi
Department of Pharmaceutical Chemistry, G. Pulla Reddy Pharmacy, Mehdipatnam, Hyderabad, Telangana, INDIA.
ABSTRACT
Background: The largest infectious agent-related cause of death and the most common disease with a high contagiousness profile is tuberculosis. For the treatment of tuberculosis, various benzimidazole and quinazoline compounds have been developed in the past with effectiveness. In this example, our goal was to synthesise new compounds with enhanced activity by combining the moieties of benzimidazole and quinazoline. The present study was planned to synthesize novel 5-(4-flourobenzoyl)12- (substitutedphenyl)-3,3-dimethyl-3,4,5,12-tetrahydrobenzo [4,5] imidazo [2,1-b] quinazolin-1(2H)-one derivatives. Materials and Methods: A series of benzamidazo quinazoline derivatives were synthesized and characterized by using IR,1 HNMR, 13CNMR, and Mass spectroscopy. The antitubercular activity of the synthesised compounds was evaluated against the H37RV strain to determine their antitubercular potential. To examine the teratogenicity of the synthesised compounds, zebrafish larvae were utilised. Results and Discussion: At 3.25 µg/ mL, compounds R2, R3, R4 and R9 exhibited good efficacy against Mycobacterium tuberculosis strains. Most of the synthesized compounds were proved as safe at 0.5 µM without any abnormalities. Conclusion: Compounds containing Electron withdrawing groups at 4th position were found to possess excellent antitubercular activity.
Keywords: Benzimidazole, Quinazoline, Antitubercular activity, Teratogenicity, Zebra fish larvae.