Title:Synthesis and Biological Evaluation of Cholic Acid Tagged Piperazine Derivatives
Volume: 28
Issue: 1
Author(s): Dima W. Alshawabkeh, Anas J. Rasras*, Saqr Abushattal, Mohammad S. Al Zubi, Mohamad M. Shakdofa, Eyad A. Younes and Raed A. Al-Qawasmeh*
Affiliation:
- Department of Chemistry, Faculty of Science, Al-Balqa Applied University, PO Box: 19117, Al-Salt, Jordan
- Department of
Chemistry, College of Sciences, University of Sharjah, Pure and Applied, Chemistry Research Group, PO Box: 27272, Sharjah, United
Arab Emirates
- Department of Chemistry, The University of Jordan, Amman 11942, Jordan
Keywords:
Antibacterial, cholic acid, heterocyclic, piperazine, MRSA, anti-COVID-19.
Abstract: Diseases caused by bacteria are a big challenge for scientists worldwide. These
bacteria can be resistant through the adaption of new ways to protect themselves against
antimicrobial drugs and thus become multidrug resistance. In this work, new derivatives of
1,3,4-oxadiazole- cholic acid were synthesized and fully characterized using different techniques,
such as 1H-NMR, 13C-NMR, and HRMS. Their biological activity, along with the
measuring of their minimal inhibitory concentration (MIC), was studied and reported. The
antimicrobial activity of the new library was assessed via in vitro screening against both
Gram-positive and Gram-negative bacteria. The compounds showed selectivity against
Gram-positive bacteria. Among the new analogues, compounds 4F and 5h were found to be
potent against S. aureus with MIC of 47 μg/mL. Compounds 4f, 5g and 5h were active
against MRSE with MIC of 188, 99, and 23 μg/mL, respectively.
