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.
Oxazolines are five-membered heterocyclic compounds with one double bond. The double bond may be in one of three positions, so there may be three different oxazoline rings. The 2-oxazoline structure is the most common, and 3-oxazoline and 4-oxazoline exist mainly as laboratory research compounds. Oxazolines exist between oxazole and oxazolidine in terms of saturation.
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