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.
Imidazolines are a class of heterocycles derived from imidazoles by reduction of one of the two double bonds. Three isomers are known, 2-imidazoline, 3-imidazoline and 4-imidazoline. 2 and 3-imidazolines contain imine centers, while 4-imidazolines contain alkene groups. The 2-imidazoline group occurs in several drugs. Imidazolines are an important class of compounds found in many natural and medicinal products. These compounds are also used as intermediates in the synthesis of organic molecules. Furthermore, chiral imidazolines are widely used as organic catalysts for the synthesis of various natural and synthetic organic compounds.
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