Synthesis and Biological Evaluation of Cholic Acid Tagged Piperazine Derivatives

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 mu g/mL. Compounds 4f, 5g and 5h were active against MRSE with MIC of 188, 99, and 23 mu g/mL, respectively.