Benzimidazole is a benzo derivative of imidazole. It is a kind of bicyclic aromatic organic compounds, which is formed by fusing a six-membered benzene ring and five-membered imidazole at positions 4 and 5 of imidazole ring. It is an important pharmacophore of many biologically active heterocyclic compounds with various pharmacological activities. Benzimidazoles and their derivatives have developed into dynamic heterocyclic systems due to their potency in a variety of biologically active compounds such as anticancer, bactericidal and antiviral drugs. Benzimidazoles are a class of therapeutic motifs with broad relevance in medicinal chemistry.
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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