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Design, synthesis, and characterization of novel substituted 1,2,4-oxadiazole and their biological broadcast

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Abstract

In the current study, a novel combinatorial library of substituted 1,2,4-oxadiazoles bearing pyridine and thiazole have been synthesized via the condensation reaction of amidoxime and carboxylic acids and its derivatives in two way. The titled compounds were screened for their in vitro antimicrobial activity against three gram positive bacteria and three gram negative bacteria, In vitro antituberculosis activity against Mycobacterium tuberculosis H37RV and in vitro antimalarial activity against Plasmodium falciparum. Majority of the compounds were found to be active against gram positive bacteria. Compounds 6e, 6f, 7e, and 7f elaborate moderate antituberculosis activity against the first-line drug while 6c, 6d, 7c, and 7d intricate excellent antimalarial activity against Plasmodium falciparum strain.

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Scheme 1
Fig. 1

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Acknowledgements

The author gratefully acknowledges the research facilities provided by the P. D. Patel Institute of Applied Sciences, CHARUSAT.

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Correspondence to Kaushal P. Patel.

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Parikh, P.H., Timaniya, J.B., Patel, M.J. et al. Design, synthesis, and characterization of novel substituted 1,2,4-oxadiazole and their biological broadcast. Med Chem Res 29, 538–548 (2020). https://doi.org/10.1007/s00044-020-02505-8

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Keywords

  • Oxadiazole
  • Pyridine
  • Thiazole
  • Plasmodium falciparum
  • Mycobacterium tuberculosis