An insight on medicinal attributes of pyrimidine scaffold: An updated review

Pyrimidine itself or in different fused forms is an important chemical motif for every step of cell life. Alongside, it exists as a key pharmacophoric part in thiamine, alloxan, orotic acid, and other isoforms of nucleotide bases. It has emerged as a privileged scaffold in medicinal chemistry due to its various possible structural and pharmacological attributes. In a number of clinically used chemical agents, pyrimidine or its fused/clubbed form with other moieties act as a key pharmacophore. Structure activity relationship (SAR) studies of the explored derivatives demonstrated that slight modifications with various substitutions on the pyrimidine rings can deviate biological activity to a large extent. 2-Pyrimidone and 2,4-pyrimidione derivatives are largely explored by a number of research groups for various pharmacological targets and due to their similarity to nucleotide bases, it has a great impact on the biological profile of these molecules. The current review focuses on describing the recent advancements (2015 onward) in the development of pyrimidine-based biologically active molecules along with drug candidates under different clinical trials. The aim of this review is to provide structural features associated with pyrimidine along with their SAR studies, which are believed to be valuable for the scientists working on the development of pyrimidine-based small molecules in the aforementioned disease conditions. We believe that the results of this research will help to provide a structural idea that may be used in the design and development of new pyrimidine-based small molecules that target a variety of receptors or enzymes.

Automated summary

Pyrimidine plays an important role in every step of cell life and has become a crucial pharmacophoric part in medicinal chemistry. It can act as a key pharmacophore in clinically used chemical agents and slight modifications on pyrimidine rings can greatly affect biological activity. This review focuses on the recent developments in pyrimidine-based biologically active molecules and provides valuable information on their structural features and structure activity relationship studies.