Benzothiazoles are aromatic heterocyclic compounds with the chemical formula C7H5NS. Benzothiazoles and their derivatives are a very important class of heterocyclic compounds that are ubiquitous in nature and are mainly used in medicine, agriculture and industry. In medicine, benzothiazole derivatives are a kind of very important pharmaceutical intermediates with good pharmacological and biological activities. It can be used as a fungicide, anti-tuberculosis drug, anti-malarial, anti-convulsant, insecticide, sedative and anti-inflammatory drug, and can also be used to treat diabetes and has anti-cancer effects.
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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