Oxadiazoles are a class of heterocyclic aromatic compounds with the molecular formula C2H2N2O, which have special biological activities and thermodynamic properties. Five-membered heterocyclic moieties composed of three or two heteroatoms are of great interest to researchers because these compounds show significant therapeutic potential. These heterocycles can serve as a building block for the development of novel molecular structures.
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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