Indole is a compound of pyrrole and benzene in parallel, also known as benzopyrrole. There are two combinations of pyrrole and benzene, called indole and isoindole, respectively. Many derivatives of indole have physiological and pharmacological activities, and can synthesize vasodilators, antihistamines, antipyretic analgesics, etc. in medicine, so indole is also a very important heterocyclic compound.
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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.
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