Synthesis, Characterization, Anti-tubercular Evaluation, and Teratogenicity Studies of Novel 5-(4-fluorobenzoyl) tetrahydro benzamidazoquinazoline Derivatives

  • 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
Keywords: Benzimidazole, Quinazoline, Antitubercular activity, Teratogenicity, Zebra fish larvae.

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

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control (b) R1 (0.5μM) (c) R2 (0.5μM) (d) R4 (0.5μM) (e) R8(0.5μM)
Published
2022-10-06
How to Cite
1.
Babu NR, Raju RS, Malothu N, Padmavathi Y. Synthesis, Characterization, Anti-tubercular Evaluation, and Teratogenicity Studies of Novel 5-(4-fluorobenzoyl) tetrahydro benzamidazoquinazoline Derivatives. ijpi [Internet]. 6Oct.2022 [cited 10Dec.2022];12(4):444-8. Available from: https://www.jpionline.org/index.php/ijpi/article/view/1693