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

Abstract

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.

Recent Advances in the Multicomponent Synthesis of Heterocycles Using 5-Aminotetrazole

“…These methods include multicomponent reactions, cyclization, and condensation reactions. [78][79][80][81][82][83][84][85][86][87] The diverse applications of 5-aminotetrazole make it a precious synthon (Figure 5).…”

Exploring the untapped pharmacological potential of imidazopyridazines

“…The biological and pharmacological properties of these analogs differ signicantly depending on their specic structure and the substitutions on the core moieties and have been reviewed thoroughly. [61][62][63][64][65] Fig. 15 Imidazopyridazine moiety in approved and investigational drugs.…”

“… 60 In addition, different analogs of imidazopyridazine with varying structural or functional similarities are known with imidazopyridazines being one of the least explored scaffolds. Some of these analogs are imidazopyridines, 61 imidazopyrizines, 62 pyrazolo[3,4- d ]pyrimidines, 63 pyrazolopyridazines, 64 pyrido[2,3- d ]pyrimidines, 65 and related structures. The biological and pharmacological properties of these analogs differ significantly depending on their specific structure and the substitutions on the core moieties and have been reviewed thoroughly.…”

Synthesis of novel pyrimido[4,5‐b]quinolines as potential anticancer agents and HER2 inhibitors

“…In addition, it is a crucial pharmacophoric component of nucleotide bases. Due to its many potential structural and pharmacological qualities, it became a preferred scaffold in medicinal chemistry (Basha & Goudgaon, 2021; Vyas et al, 2022). Pyrimidines have established and exhibit strong activity against breast cancer (Luo et al, 2018; Scherbakov et al, 2018; Wang et al, 2018).…”