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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The molecular structure of cyclobutane has four carbon atoms, and its four carbon atoms are not in the same plane, which is the folded conformation of cyclobutane. Cyclobutane itself is not of commercial or biological interest, but more complex derivatives are important in biology and biotechnology. Currently, nine FDA-approved drugs contain the cyclobutane structure. From the perspective of therapeutic areas, cyclobutyl drugs are mainly distributed in popular areas such as tumors, neurological diseases, infectious diseases, endocrine and metabolic diseases.
Thiadiazoles are a subfamily of azoles. Structurally, they are five-membered heterocyclic compounds containing two nitrogen atoms and one sulfur atom, and two double bonds, forming an aromatic ring. Depending on the relative positions of the heteroatoms, there are four possible structures; these forms do not interconvert and are therefore structural isomers rather than tautomers. These compounds themselves are rarely synthesized and have no particular utility, however, compounds that use them as structural motifs are fairly common in pharmacology.
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