Hybridization of Fluoroquinolones as a Promising Pathway towards New Antibiotics ^†

Abstract

The current situation in medicine and pharmacy still requires the time and effort of medicinal chemists, who must develop new synthetic approaches and create promising molecules that can turn into novel antimicrobials. Due to the problem of resistance to well-known antibiotics combined with the occurrence of new diseases that we observe, we can be sure that this research is going to be in demand. However, not always searching for a totally new molecule seems to be a good idea. The structural modification and hybridization of once efficient agents is also logical and actually has already provided us with many generations of antibiotics. Therefore, our scientific team has been working with fluoroquinolones with the aim of conducting docking studies, modifying them, and then studying the biological activity of the obtained compounds. In the first stage of the research, we conducted docking studies and then started to work on ciprofloxacin and norfloxacin, only modifying their C-7 position. The introduction of a 1,2,3-triazole moiety as a result of a convenient synthetic procedure led to new molecules for which moderate antimicrobial and antifungal activities were revealed. Furthermore, the C-3 position was modified with an arylsulfonyl moiety with parallel modifications of N-1 and C-7. For now, synthetic procedures have been developed for the similar transformation and biological activity of the obtained compounds that are under study.