Hybridization of Fluoroquinolones as a Promising Pathway towards New Antibiotics

Current situation in medicine and pharmacy still requires 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 these researches are going to be in demand.

However, not always searching for a totally new molecule seems to be a good idea. 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 aiming to conduct docking studies, modify them, and then study biological activity of the obtained compounds.

At the first stage of the research we conducted docking studies and then started to work on ciprofloxacin and norfloxacin, modifying only their C-7 position. Introduction of 1,2,3-triazole moiety as a result of a convenient synthetic procedure led to new molecules for which moderate antimicrobial and antifungal activities was revealed. Furthermore, C-3 position was modified with arylsulfonyl moiety with parallel modifications of N-1 and C-7. For now, synthetic procedures are developed for similar transformation and biological activity of the obtained compounds is under study.