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.
Compared to quinolines, isoquinolines are also prominent structural motifs present in many biologically significant natural and synthetic compounds. Some well-known isoquinoline alkaloids include the anticancer and anticonvulsant berberine, the vasodilator and antispasmodic drugs papaverine and emetine. In addition to naturally occurring isoquinolines, synthetic analogs have also shown significant biological activity.
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