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.
Benzotriazole is a bicyclic nitrogen heterocycle formed by the fusion of the benzene ring with the 4,5-positions or the “d” site of 1H-1,2,3-triazole. The benzotriazoles are known as important intermediates in the preparation of organic products such as β-amido ketones, aldehydes, β-ketoesters, ionic liquid, and as reagents for acylation and thioacylation reactions. 1H-Benzotriazoles are also known to exhibit broad spectrum of pharmacological activities. There are numerous benzotriazole-based clinically used drugs in the market for the treatment of various diseases.
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