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.
Naphthyridine is a class of aromatic heterocyclic compounds whose chemical formula is C8H6N2. They consist of naphthalene bicyclic rings in which two carbon atoms are replaced by nitrogen atoms. There are ten isomers of naphthyridine, because naphthyridine has two benzene rings, has strong π-π conjugation, and has better luminescence properties. Common naphthyridines are 1,8-naphthyridines. There are many kinds of 1,8-naphthyridine derivatives, and they are widely used.
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