In recent years, plenty of research has been aimed at the multiple properties of different carbazole derivatives. Carbazoles are important aromatic heterocyclic compounds isolated from plants, such as those of the genera Ochrosia, Murraya, Glycosmis, and Clausena, or synthetically obtained. Today, many carbazole derivatives are widely studied as photoconductive, anti-bacterial, anti-fungal, anticancer, antioxidant, anti-inflammatory, anti-Alzheimer, anti- malarial, anti-tuberculosis, and anti-viral agents, for the treatment of obesity and for their psychotropic and antihistamine activities. However, the therapeutic applications and benefits of some of these derivatives remain low because of their low hydrosolubility, low bioavailability, and the onset of some side effects. For these reasons, the purpose of this Special Issue "Carbazole Derivatives: Latest Advances and Prospects" is to report the molecular modeling, synthesis, and biological evaluation of new carbazole derivatives with improved pharmacokinetic and pharmacodinamic properties for their development in medicinal chemistry.