Background: The quinoline ring system is one of the most commonly encountered heterocycles
in medicinal chemistry, due to the pharmaceutical and medicinal uses of derivatives containing
this ring. These quinoline-based compounds have remarkable biological activity, as they are
employed as antimalarial, antibacterial, antifungal, and antitumor agents. The quinoline nucleus
can be synthesized by various traditional methods such as the Skraup reaction, Friedlaender synthesis,
Combes quinoline synthesis, Larock quinoline synthesis, among others.
Methods: The aim of the present work is to synthesize a number of new arylated quninolines having
significant antinoceciptive effect through the Suzuki-Miyaura cross coupling reaction using 3-
bromoquinoline as a starting material.
Results: A number of new quinoline derivatives have been synthesized. Structures of the newly synthesized
compounds were confirmed by means of IR, NMR, and mass spectrometry, and by elemental
analysis. In addition, the molecular structures of two representative derivatives were determined with
the aid of X-ray crystallography. Additionally, the antinociceptive activity of the prepared compounds
was evaluated in vivo; results revealed that most of the tested compounds exhibited a dosedependent
Conclusion: Prepared compounds were found to exhibit significant antinociceptive activities and
could be used as potential analgesic agents. Further work, however, may be required to establish
the safety and efficacy of these compounds.