Synthesis of 8‐Hydroxy Quinoline Derivatives: A Revolutionary Target in Medicinal Chemistry (2020–2025)

Abstract A wide range of pharmaceutical compounds incorporate the quinoline ring, a flexible heterocyclic framework often regarded as a “privileged scaffold” in the search for new therapeutic agents. Among its notable derivatives is 8‐hydroxyquinoline (8‐HQ), commonly referred to as oxine. It is considered a groundbreaking target in medicinal chemistry because of its significant biological activity and logical design. The synthetic modification of 8‐hydroxyquinoline is the subject of extensive investigation in an effort to develop more potent target‐based, wide‐ranging medicinal compounds. This review summarizes recent advancements ( 2020 – 2025 ) in the development of 8‐hydroxyquinoline derivatives, emphasizing their diverse pharmaceutical potential, including anti‐proliferative, anticancer, antibacterial, antimicrobial, antifungal, antiviral, and other pharmacological activities documented in literature from 2020 to 2025. The goal is to help medicinal chemists investigate and create new congeners with better biological activity and stronger target‐based broad‐spectrum therapeutic molecules with fewer side effect risks for the treatment of a number of serious illnesses.