Azetidines are an important class of saturated four-membered nitrogen-containing heterocyclic compounds. The research hotspots related to this structure mainly focus on two aspects: one is the research of pharmaceutical chemistry; the other is related to chiral azetidines, using rigid azetidine compounds as chiral ligands for asymmetric catalytic reactions. Many nitrogen-containing heterocycles play important roles in drug structures, and in many cases small structural changes can improve ligand selectivity and pharmacokinetic properties.
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Cyclopropane is the smallest cyclic compound with unique structural features and physicochemical properties, which is widely used in the design of small molecule drugs. In drug design, it is often used to increase activity, fix conformation and improve PK and water solubility. The introduction of cyclopropyl groups into drugs can change various properties of molecules, such as improving metabolic stability; increasing biological activity; enhancing drug efficacy; limiting polypeptide conformation and slowing down its hydrolysis; reducing plasma clearance; improving drug dissociation and many more. Cyclopropane rings are widely found in marketed drugs, including cardiovascular drugs, central nervous system (CNS) drugs, anticancer drugs, autoimmune and anti-inflammatory drugs.
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