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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1,2-Benzoisoxazole is an aromatic organic compound with the molecular formula C7H5NO containing a benzene-fused isoxazole ring structure. The compound itself has no general application; however, functionalized benzoxazoles and benzoisoxazoles have a variety of uses, including therapeutic drugs such as some antipsychotics (including risperidone, paliperidone, cape ketone and iloperidone) and the anticonvulsant azolamide.
The use of azepane as a scaffold for drug discovery remains of interest. The azepane linker is the key to efficient activity. A number of seven-membered ring derivatives have been prepared or investigated for their potential or actual pharmacological properties. Examples include azaalkane derivatives as PKB (protein kinase B) inhibitors.
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