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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Benzimidazole is a benzo derivative of imidazole. It is a kind of bicyclic aromatic organic compounds, which is formed by fusing a six-membered benzene ring and five-membered imidazole at positions 4 and 5 of imidazole ring. It is an important pharmacophore of many biologically active heterocyclic compounds with various pharmacological activities. Benzimidazoles and their derivatives have developed into dynamic heterocyclic systems due to their potency in a variety of biologically active compounds such as anticancer, bactericidal and antiviral drugs. Benzimidazoles are a class of therapeutic motifs with broad relevance in medicinal chemistry.
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