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Sulfonyl-Benzoxazole Based 1,2,4-Oxadiazoles: Synthesis, In Vitro Antibacterial, Antibiofilm, and In Silico ADME Studies

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Abstract

In search of the better antibacterial agents, a series of novel new 2-(((5-aryl-1,2,4-oxadiazol-3-yl)methyl)sulfonyl)benzo[d]oxazole derivatives were synthesized using 2-(benzo[d]oxazol-2-ylsulfonyl)acetonitrile and readily available aromatic carboxylic acids. The newly synthesized derivatives were evaluated for their in vitro antibacterial activity against G+ve strains. 2-(((5-(4-fluorophenyl)-1,2,4-oxadiazol-3-yl)methyl)sulfonyl)benzo[d]oxazole showed significant activity against B. subtilis, which is two times higher than that of ciprofloxacin. Anti-biofilm activity results reveled that, 2-(((5-(4-fluorophenyl)-1,2,4-oxadiazol-3-yl)methyl)sulfonyl)benzo[d]oxazole and 4-(3-((benzo[d]oxazol-2-ylsulfonyl)methyl)-1,2,4-oxadiazol-5-yl)benzonitrile shows effective inhibitors of biofilm growth. Molecular docking and ADME studies have also been conducted to complement the experimental results.

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ACKNOWLEDGMENTS

The authors are thankful to the head, Department of Biotechnology, Kakatiya University, Warangal, for providing data of biological activity.

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  1. Department of Chemistry, JNTUH, College of Engineering, 505501, Nachupally, Kondagattu, Jagtial, Telangana, India

    K. Vidya

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  1. K. Vidya
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Correspondence to K. Vidya.

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Vidya, K. Sulfonyl-Benzoxazole Based 1,2,4-Oxadiazoles: Synthesis, In Vitro Antibacterial, Antibiofilm, and In Silico ADME Studies. Russ J Bioorg Chem 48 (Suppl 1), S101–S109 (2022). https://doi.org/10.1134/S1068162023010272

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