Pyrans are an important class of six-membered heterocyclic compounds, non-aromatic rings, composed of five carbon atoms and one oxygen atom, and contain two double bonds. The molecular formula of pyran is C5H6O, and there are two isomers. Pyrans, together with benzo derivatives, form scaffolds for a variety of drug applications, many of which are approved and promising candidates in clinical trials and recently isolated bioactive natural products.
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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