Benzimidazole is a benzo derivative of imidazole. It is a kind of bicyclic aromatic organic compounds, which is formed by fusing a six-membered benzene ring and five-membered imidazole at positions 4 and 5 of imidazole ring. It is an important pharmacophore of many biologically active heterocyclic compounds with various pharmacological activities. Benzimidazoles and their derivatives have developed into dynamic heterocyclic systems due to their potency in a variety of biologically active compounds such as anticancer, bactericidal and antiviral drugs. Benzimidazoles are a class of therapeutic motifs with broad relevance in medicinal chemistry.
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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