: Naphthyridine is the class of aromatic heterocyclic compounds which are subgroup of diazanaphthalene. To our knowledge and search from this work perspective, six naphthyridine drugs were  found around (enoxacin, nalidixic acid, trovafloxacin, alatrofloxacin, gemifloxacin and pyronaridine) that are therapeutically approved; these drugs are useful in the management of bacterial infections and pyronaridine is useful in malarial therapy. There were also several patents of naphthyridines as potential drugs and intermediates. We also came across some of naphthyridine derivatives that are in the clinical trial phases. Even though naphthyridine derivatives are versatile molecules that exhibit a variety of pharmacological activities and biological effects; in our extensive literature search, we did not encounter comprehensive review reports on naphthyridine derivatives. There were review reports available about some of the drugs (naphthyridines) clinically approved and under trials, these were mostly oriented towards a single chemical entity. This lead to conceptualize the present compilation of the most significant research literature available on naphthyridine derivatives. This compilation intends to be a major single source of information of several chemical derivatives of naphthyridine that are screened for pharmacological and biological activities. Naphthyridines derivatives exhibit various biological and pharmacological activities which includes antimicrobial (antibacterial, antifungal, antiviral & antimalarial), anti-leishmanial, immunomodulatory, analgesic, anti-inflammatory, anti-alzheimer, anti-vertigo, anticonvulsant, cardiovascular (antiarrhythmic, antihypertensive, α-receptor antagonist & β-blocker), anticancer, diuretic, gastric anti-secretary, bile acid transport inhibitory, antioxidant and phytocytotoxicity activity. In this review article, we have attempted to compile the most significant reports of biological and pharmacological activities of naphthyridine derivatives available literature from 1970 to 2020.

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