Abstract: Piperidine and pyridine nuclei are essential heterocyclic systems and act as an essential underpinning for agriculture, medicines, industries, etc. The development of novel methods for the synthesis of these exemplary heterocyclic compounds and their respective hybrids, which show a wide range of biological activities, is a very fascinating theme. The derivatives of these pervasive nuclei are used as antibacterial, antimicrobial, antifungal, antimalarial, anticancer, antiproliferative, antihypertensive, antiparasitic, and many other agents. The hybrids of these nuclei have retained a distinct position in medicinal chemistry and are often incorporated in synthetic drug discovery. In this review, we have compiled relevant literature on different derivatives of piperidine and pyridine moieties and their biological activities.