Abstract

and 28b were predicted to bind S. aureus MurC ligase. The 23a and 28b formed bonds with MurC residues at binding site, specifically Ser12 and Arg375, indicating consequential interactions essential for complex stability. The in vitro antimicrobial activity of compound 28b was not affected by the addition of 50% serum. Finally, all tested bis(thia- zol-5-yl)phenylmethane derivatives showed favorable cytotoxicity profiles in A549 and THP- 1-derived macrophage models. These results demonstrated that bis(thiazol-5-yl)phenyl- methane derivatives 23a and 28b could be potentially explored as scaffolds for the develop- ment of novel candidates targeting drug-resistant S. aureus. Further studies are also warranted to understand in vivo safety, efficacy, and pharmacological bioavailability of bis (thiazol-5-yl)phenylmethane derivatives.