Enzyme inhibition and antibacterial potential of 4-Hydroxycoumarin derivatives

Authors

  • Afia Saleem COMSATS University Islamabad, Department of Chemistry
  • Syed Majid Bukhari COMSATS University Islamabad, Department of Chemistry
  • Asma Zaidi COMSATS University Islamabad, Department of Chemistry
  • Umar Farooq COMSATS University Islamabad, Department of Chemistry
  • Majid Ali COMSATS University Islamabad, Department of Chemistry
  • Asma Khan Fujian Institute of Research on Structure of Matter Chinese Academy of Science
  • Sidra Khan Schanghai Jiao Tong University, School of Chemistry and Chemical Engineering
  • Kausar Hussain Shah Bahauddin Zakariya University, Institute of Pure and Applied Biology
  • Adeem Mahmood King Saud University, College of Science, Department of Chemistry https://orcid.org/0000-0001-7732-5645
  • Farhan Ahmed Khan COMSATS University Islamabad, Department of Chemistry

DOI:

https://doi.org/10.1590/s2175-97902019000418654

Keywords:

4-Hydroxycoumarin, Anti-urease, Carbonic anhydrase, Aldehydes, Antibacterial

Abstract

The 4-Hydroxycoumarin derivatives are known to show a broad spectrum of pharmacological applications. In this paper we are reporting the synthesis of a new series of 4-Hydroxycoumarin derivatives synthesized through Knovenegal condensation; they were characterized by using UV-Vis, FT-IR, NMR spectroscopies. The synthesized compounds were evaluated for antibacterial activity against Staphylococcus aureus and Salmonella typhimurium strains. The compounds (2), (3) and (8) showed favorable antibacterial activity with zone of inhibitions 26.5± 0.84, 26.0 ± 0.56 and 26.0 ± 0.26 against Staphylococcus aureus (Gram-positive) respectively. However, the compounds (5) and (9) were found more active with 19.5 ± 0.59 and 19.5 ± 0.32 zone of inhibitions against Salmonella typhimurium (Gram-negative). Whereas, in urease inhibition assay, none of the synthesized derivatives showed significant anti-urease activity; although, in carbonic anhydrase-II inhibition assay, the compound (2) and (6) showed enzyme inhibition activity with IC50 values 263±0.3 and 456±0.1, respectively.

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Published

2021-03-02

How to Cite

Saleem, A. ., Bukhari, S. M. ., Zaidi, A. ., Farooq, U. ., Ali, M. ., Khan, A. ., Khan, S. ., Shah, K. H. ., Mahmood, A. ., & Khan, F. A. . (2021). Enzyme inhibition and antibacterial potential of 4-Hydroxycoumarin derivatives. Brazilian Journal of Pharmaceutical Sciences, 56, e18654 . https://doi.org/10.1590/s2175-97902019000418654

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