Thiophene is a five-membered heterocyclic compound containing a sulfur heteroatom with the molecular formula C4H4S. Thiophene is aromatic and is very similar to benzene; electrophilic substitution reaction is easier than benzene, and it is mainly substituted at the 2-position. Thiophene ring system has certain stability to oxidant.
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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