AbstractLife of the living organism is based on phosphorous, and it is involved in almost all important biological and biochemical processes such as energy transfer, bone development and storing genetic information. Many of the therapeutic agents having C─P bond, isolated naturally as well and widely used in daily clinical practices are phosphorus‐containing drugs (e.g: phosphotriesters, phosphonates, phosphinates, phosphine oxides, phosphoric amides, bisphosphonates, phosphoric anhydrides, etc.) and growing further. The phosphorus heterocycles (PHs) integrate the merits of both phosphorus atom and heterocyclic scaffolds representing an important class of organophosphorus compounds, which are constantly drawing the attention among both industrial and scientific society as these compounds have shown varieties of related applications. Owing to its seminal biological importance PHs have inspired a whole generation of medicinal chemists to come up with novel scaffolds containing phosphorous atom. This review is focused mainly on the compilation of different classes of bioactive phosphorus containing heterocyclic skeletons (which includes phosphorus atom within the heterocyclic ring system or as substituted phosphorus atom attached with another heterocyclic ring system) having both therapeutic and other material chemistry applications since the year 2000 onwards barring their synthetic routes.
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