Privileged heterocyclic scaffolds in chemical biology and drug discovery: synthesis and bioactivity

The impressive advances in the ability of organic and medicinal chemists to efficiently prepare libraries containing thousands of small organic molecules has allowed, in the last two decades, to generate molecular tools with proven utility in understanding complex biological processes and unraveling molecular dysfunctions underlying diseases, ultimately contributing to improve strategies and tools in drug discovery processes. Nevertheless, high-throughput screening of molecular libraries, through biochemical assays, often proves disappointing due to the poor specificity and utility of the compounds discovered, with a negative impact on costs, in terms of time and resources employed.