Design, Synthesis and Anti-Bacterial Activity Evaluation of Indole-Based Benzophenone and Their Derivatives

Year 2023, Volume: 10 Issue: 3, 653 - 658, 30.08.2023

Fekadu Tumoro Erabe Dagne Adisu Kure Salah Sherif

https://doi.org/10.18596/jotcsa.1235642

Abstract

Indole and benzophenone moiety are of significant interest to investigators because they are found in many natural products and pharmacologically active compounds. They represent versatile synthetic building blocks. The benzophenone and indole scaffolds are special structures in medicinal chemistry because these compounds are found in several biologically active natural products, compounds containing indole and benzophenone exhibit anticancer, antiinflammatory, antimicrobial, and antiviral activities. In this study, derivatives of 2-(diphenyl methylene) hydrazine, containing both indole and benzophenone moieties were successfully synthesized. The structural elucidation of the synthesized compounds were done using spectroscopic techniques like IR, 1HNMR, and 13CNMR. The synthesized target compounds were investigated for their in vitro antibacterial activity against two bacterial strains; staphylococcus aureus (S. auras), and Escherichia coli (E. coli) using the disc diffusion method. All synthesized target compounds showed no significant activity against Staphylococcus aureus (S. aureus) but exhibited moderate activity against Escherichia coli (E. coli). Among all the synthesized compounds, 2-(diphenyl methylene)-1-((1-tosyl-1H-indol-3-yl) methylene) hydrazine (BHT) (7b) showed a good inhibition at a concentration of 50 μg/mL with a zone of inhibition of 21.7 mm against Escherichia coli (E.coli) which was comparable with standard drug Ceftriaxone with the zone of inhibition of 26 mm. Thus, this compound could be considered as a lead molecule to design and develop novel antibacterial drugs.

Keywords

antibacterial, benzophenone, indole, synthesis

Thanks

The author thanks Hawassa University for their financial support. The authors are also thankful to the Department of Chemistry for providing research facilities to complete this work.

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