With four imidazopyridine-containing drugs and one pyrazolopyridine-containing drug on the market, bicyclic pyridines containing ring-junction nitrogen are privileged structures in medicinal chemistry. With two nitrogen atoms with potential to serve as hydrogen bond acceptors, imidazopyridines and pyrazolopyridines may boost binding to target proteins and elevate potency. In addition, these structures have found utility in FBDD, covalent inhibitors, reducing metabolic liabilities, and creating novel chemical space and intellectual properties. With many of the advanced intermediates now commercially available, they will find more and more applications in drug discovery.
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Tetrazoles are doubly unsaturated five-membered aromatic heterocycles consisting of one carbon atom and four nitrogen atoms. Tetrazole derivatives are a major class of heterocyclic compounds that are important for medicinal chemistry and drug design because of their not only isosteric properties with carboxylic acid and amide moieties, but also metabolic stability and other beneficial physicochemical properties.
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