In the Nonclassical Biological Activities of Quinolone Derivatives published in Journal of Pharmacy & Pharmaceutical Sciences Vol 15, No 1 2012, it outlines why the quinolones are an excellent platform (scaffold) for modification to create new pharmaceuticals.
The Journal states “Quinolones as “privileged building blocks” with simple and flexible synthetic routes allow the production of large libraries of bioactive molecules. Because of their diversity, drug-like properties and similarities to specific targets they are considered a central scaffold to build chemical libraries with promising bioactivity potential.”(1)
As I have discussed before, the quinolone family of drugs show biological activity in three areas antibacterial, anticancer, and antiviral. Plus its scaffold, or its molecular structure, allows researchers to make structural modifications to transform from an antibacterial into an anticancer agent and/or an antiviral agent.
Since our focus is one of public safety, it behooves us to monitor the research world for the creation, testing, and ultimate release of quinolone derivatives into the marketplace. It is this author’s opinion, that anything based on the quinoline pharmacophore synthetic or not, whose history can be traced all the way back to the cinchona tree, has a unique propensity for toxic damage in the human body. A propensity not full realized or understood by researchers.
As of May, 2016 the Pew Charitable Trusts listed 37 antibiotics in clinical development. Of the 37 new antibiotics listed 6 were either fluoroquinolone or quinolone based.
WCK2349 a novel sub-class of the quinolone benzoquinolizine fluoroquinolone levonadifloxacin
WCK771 a novel sub-class of the quinolone benzoquinolizine fluoroquinolone levonadifloxacin
Currently in Phase 2 Development
Finafloxacin a novel member of the fluoroquinolone class
Nemonoxacin a novel nonfluorinated quinolone
Currently in Phase 3 Development
Zabofloxacin a novel member of the fluoroquinolone class
Baxdela (delafloxacin) a novel member of the fluoroquinolone class
Again, it is this author’s opinion that researchers start from a flawed premise when developing quinolones. That flawed premise is that the quinolones have a good safety profile. They generally do not take into consideration factors such as delayed toxicity and mitochondrial toxicity. According to mitochondrial researchers most of the frequently prescribed fluoroquinolones are mito toxic.(2)
It is interesting to note that some of these newer quinolones are using some novel modifications to manipulate efflux pumps that are associated with bacterial resistance. It has been speculated in the past that eukaryotic efflux pumps (as opposed to bacterial efflux pumps) may play a role in adverse events.
As we know many of the supposedly safe quinolones have been removed due to toxicity issues. In addition, the ones that currently remain on the market, that are deemed safe by the FDA and the medical community, have serious safety concerns. For this reason we must stay vigilant to the release of new quinolones that have the propensity to affect public safety.
I will continue to write about these quinolones as research data becomes available.
Stayed tuned to My Quin story for updates on community related research information.
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