Pyrazolopyrimidines as attractive pharmacophores in efficient drug design: A recent update

Abstract

Among the menacing diseases, cancer needs the most attention as millions of people are affected by it worldwide. Genetic and environmental factors play a pivotal role in causing cancer. Although a wide range of underlying mechanisms of cancer has been discovered, efficient treatments have not been discovered to date. Additionally, diseases caused by microbes such as viruses, bacteria, protozoa, and so forth, persistently result in several deaths. Also, inflammation is a major factor that leads to several health issues. For decades, drug design has become a major part of drug discovery and development for curing various diseases. Among the large number of pharmacological agents that have been synthesized, only very few have emerged as efficient drug molecules. Most of them are heterocyclic compounds, which are promising candidates for the design of efficient drug molecules. Furthermore, fused heterocycles showed comparatively stronger pharmacological activities than monocyclic heterocycles. The literature reveals that pyrazolopyrimidines have outstanding biological activity. Hence, here, the diverse pharmacological activities shown by pyrazolopyrimidine derivatives reported in the last 5 years are collated and reviewed systematically. This review is classified into various sections focusing on anticancer, antimicrobial, anti-inflammatory, and enzyme inhibitors.Structure-activity relationships are discussed in brief, which will help researchers design potent pharmacological agents.

Synthesis and Molecular Docking Study of Novel Pyrimidine Derivatives against COVID-19

“…Several synthetic molecules containing heterocyclic moieties are currently known for their antiviral potentials [ 6 , 7 , 8 , 9 , 10 , 11 ]. Pyrazolo[3,4- b ]pyridine nucleus is an important scaffold in a variety of marketed anxiolytic antidepressant drugs such as cartazolate, tracazolate and etazolate ( Figure 1 ).…”

Interaction Patterns of Pyrazolopyrimidines with Receptor Proteins

“…Pyrazolo­[3,4- d ]­pyrimidines are the most studied isomer, which are reported to have anticancer activity, , antimicrobial activity, , anti-inflammatory activity , and activity toward adenosine receptors, xanthine oxidase, and growth factor receptor kinases . Specific carbon and nitrogen atoms of the pyrazolo­[3,4- d ]­pyrimidines scaffold, vital for its anticancer and antimicrobial activities, have also been identified. , As Pyp rings are privileged scaffolds in medicinal chemistry, which can bind to diverse receptors, the broad spectrum of medicinal properties documented for their derivatives is unsurprising. , …”

“…6,11 As Pyp rings are privileged scaffolds in medicinal chemistry, which can bind to diverse receptors, the broad spectrum of medicinal properties documented for their derivatives is unsurprising. 12,41 In silico structure−activity studies and molecular docking have a significant share in the rich scientific literature on the biological activities of pyrazolopyrimidines. As the receptor binding of ligands is often dominated by molecular interactions of the functional groups attached to a core scaffold, the interactions originating from the core scaffold are undervalued in an in silico docking analysis.…”