5-Oxo-hexahydroquinoline (5-oxo-HHQ) represents a biologically attractive fused heterocyclic core. Various synthetic analogs of 5-oxo-HHQ have been synthesized and assessed for different biological activities. Some derivatives have exhibited myorelaxant, analgesic, anticancer, antibacterial, antifungal, antitubercular, antimalarial, antioxidant, anti-inflammatory, multidrug resistance reversal, anti-Alzheimer, neuroprotective, antidiabetic, antidyslipidemic and antiosteoporotic activities. This review provides a comprehensive report regarding the preparation and pharmacological characterization of 5-oxo-HHQ derivatives that have been reported so far. This information will be beneficial for medicinal chemists in the field of drug discovery to design and develop new and potent therapeutical agents bearing the 5-oxo-HHQ nucleus.
Keywords: 5-Oxo-hexahydroquinoline; Anticancer; Biological effects; Medicinal chemistry; Multicomponent reaction; Structure–activity relationship.