Benzoisothiazole is a benzo derivative of isothiazole, which is a kind of bicyclic aromatic organic compound, which is formed by fusion of a six-membered benzene ring and a five-membered heterocyclic ring composed of two adjacent heteroatoms, N and S. Benzoisothiazoles are important pharmaceutical intermediates. Some benzoisothiazole derivatives exhibit potent cytotoxic and antitumor activities.
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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