Synthesis and Biological Evaluation of Cholic Acid Tagged Piperazine Derivatives-Reference-Cited by-同舟云学术

Synthesis and Biological Evaluation of Cholic Acid Tagged Piperazine Derivatives

Published:2024-01 Issue:1 Volume:28 Page:65-73
ISSN:1385-2728
Container-title:Current Organic Chemistry
language:en
Short-container-title:COC

Author:

Alshawabkeh Dima W.¹,Rasras Anas J.¹,Abushattal Saqr²,Al Zubi Mohammad S.¹,Shakdofa Mohamad M.³⁴,Younes Eyad A.⁵,Al-Qawasmeh Raed A.⁶⁷

Affiliation:

1. Department of Chemistry, Faculty of Science, Al-Balqa Applied University, PO Box: 19117, Al-Salt, Jordan

2. Department of Biology, Al-Hussein Bin Talal University, Ma'an, Jordan

3. Inorganic Chemistry Department, National Research Center, El-Bohouth St, Dokki, Cairo, Egypt

4. Department of Chemistry, College of Science and Arts at Khulais, University of Jeddah, Jeddah, Saudi Arabia

5. Department of Chemistry, Faculty of Science, The Hashemite University, PO Box: 330127, Zarqa 13133, Jordan

6. Department of Chemistry, College of Sciences, University of Sharjah, Pure and Applied, Chemistry Research Group, PO Box: 27272, Sharjah, United Arab Emirates

7. Department of Chemistry, The University of Jordan, Amman 11942, Jordan

Abstract

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.

Funder

Deanship of Scientific Research, Al-Balqa Applied University

Publisher

Bentham Science Publishers Ltd.

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