Indole is a compound of pyrrole and benzene in parallel, also known as benzopyrrole. There are two combinations of pyrrole and benzene, called indole and isoindole, respectively. Many derivatives of indole have physiological and pharmacological activities, and can synthesize vasodilators, antihistamines, antipyretic analgesics, etc. in medicine, so indole is also a very important heterocyclic compound.
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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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