A Comprehensive Review: Bio-Potential of Barbituric Acid and its Analogues

Abstract

In our present work, we emphasized on the potential of barbituric acid (1) derivatives as drugs like anti-bacterial, hypnotic, sedative, anti-microbial and antifungal agents. As naturally occurring, barbituric acid (1) is inactive but in the derivative form, it has a large number of medicinal uses and nowadays, it has a great demand in the pharmaceutical industry. Barbituric acid has a wide range of applications in the synthesis of a diverse class of compounds like heterocyclic, carbocyclic, synthetic alkaloids, and due to its broad-spectrum applications, barbituric acid acquired the position of building blocks in synthetic chemistry. Through the history of humanity, a number of bioactive agents have been applied to cure the disease related to hypnotics and sedatives, while the exact efficacy of these agents was found to be limited. Till now, review articles on barbituric acid only express their specific aspect but in present review article, all aspects are discussed in detail to provide a platform to readers and researchers so that they could obtain all information and background knowledge from a single point.

Enantioselective Synthesis of Spiro Heterocyclic Compounds Using a Combination of Organocatalysis and Transition‐Metal Catalysis

“…Conversely, Vitale used the procedure for synthesizing spirocyclopentanes bearing barbituric acid 13, which is known for its therapeutic value, and its derivatives are widely used in medicine. [49,50] Corresponding spirobarbituric acid 13 was isolated under optimized conditions in the yield of 67 % with good diastereoselectivity (81 : 19 dr) and with high level of enantiomeric purity (99.5 : 0.5 er).…”

Boosting the Discovery of Small Molecule Inhibitors of Glucose-6-Phosphate Dehydrogenase for the Treatment of Cancer, Infectious Diseases, and Inflammation

“…The scaffold of pyrimidine-2,4,6­(1 H ,3 H ,5 H )-trione is present in barbiturates, and this structural feature may cause off-target effects; barbiturates elicit their sedative effect by acting on GABA A receptors in the mammalian central nervous system. However, what renders barbiturates active is the appropriate substitution at the carbon between the two carbonyl functionalities . In the projected structures 11a – c (Figure ), that carbon is substituted with an alkylidene moiety and, therefore, the resulting acrylamide moiety renders the molecules as potential Michael acceptors.…”

“…However, what renders barbiturates active is the appropriate substitution at the carbon between the two carbonyl functionalities. 52 In the projected structures 11a−c (Figure 6), that carbon is substituted with an alkylidene moiety and, therefore, the resulting acrylamide moiety renders the molecules as potential Michael acceptors. Upon exposure to GSH or cysteine, compounds of type 15 can be obtained, suggesting the potential to react with cysteines present in G6PD.…”

Iodine-Catalyzed Multicomponent Synthesis of Highly Fluorescent Pyrimidine-Linked Imidazopyridines

“…Similar to imidazopyridines, the pyrimidine moiety, especially barbituric acid and its derivatives, is an important pharmacophore and exhibits diverse medicinal properties. 12 The design and synthesis of hybrid molecules bearing more than one pharmacophore has gained considerable interest in recent times. 13 Considering the importance of hybrid molecules, imidazopyridines and the pyrimidine moiety, and in continuation of our work on the development of new methodologies, 14 we turned our attention to developing a new metal-free methodology for the synthesis of pyrimidine-linked imidazopyridines from the readily available starting materials.…”

“…Similar to imidazopyridines, the pyrimidine moiety, especially barbituric acid and its derivatives, is an important pharmacophore and exhibits diverse medicinal properties . The design and synthesis of hybrid molecules bearing more than one pharmacophore has gained considerable interest in recent times .…”