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.
Oxygen heterocycles are one of the most common heterocycles in drugs and natural products. Oxetene has high polarity and is also a good acceptor for hydrogen bond, which contributes to the metabolism and chemical stability of its host molecules. When substituted for commonly used functional groups such as gem dimethyl or carbonyl, oxetane units can induce profound changes in water solubility, lipophilicity, metabolic stability and conformational preference. Four of the FDA-approved drugs contain oxetenes: Orlistat, Paclitaxel, and two of its derivatives, Docetaxel and Cabazitaxel. Currently, oxetane-containing building blocks are flourishing in medicinal chemistry and drug discovery.