Quinolones: Chemistry and Biological Activities

Dear colleagues,

Quinolones represent a highly important class of synthetic antibacterial agents and received special attention in drug discovery. Developed in 1962, nalidixic acid, derived from chemical modifications of a by-product of the chloroquine synthesis, was the first quinolone approved for clinical use. Proper functionalization of the quinolone core can originate compounds endowed with a variety of biological activities including anticancer, antitubercular, antiviral, antimalarial, and anti-Alzheimer activities. Quinolones exert their antimicrobial activity by forming a ternary complex with DNA gyrase or Topoisomerase IV and bacterial DNA. In a similar manner, the anticancer activity is likely due to the formation of the ternary complex represented by quinolone/human Topoisomerase II/DNA.

In the last ten years, the two molecules vosaroxin and enoxacin have attracted much attention. Vosaroxin is currently in Phase III clinical trial as anticancer agent while enoxacin represents the first-in-class RNA interference enhancer molecule acting through the interaction with TAR-RNA binding protein, a co-factor involved in dicing activity of DICER. Beside the biological activities, the great importance of quinolones in the medicinal chemistry field has also driven the research towards the application of new and greener synthetic approaches.

In this Special Issue, we aim to collect a series of high-quality reviews and original papers spanning from chemical synthesis, drug repositioning of old quinolones, design of new molecules, analytical determination in the ecosystem, biological evaluation and last but not least toxicology aspects. We are proud to invite you to submit your own contribute on the Special Issue: “Quinolones: chemistry and biological activities”.

Prof. Giuseppe Manfroni
Dr. Tommaso Felicetti
Guest Editors

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