Cyclohexane is an organic compound with a chemical formula C6H12. It is a colorless liquid with a pungent odor, insoluble in water, and soluble in most organic solvents such as ethanol, ether, benzene, and acetone. Cyclohexyl fragments are a common structure in both natural and synthetic drugs. It can be used as both core structure and part of achiral side chain.
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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