Piperidine is an azacycloalkane that is cyclohexane in which one of the carbons is replaced by a nitrogen. Although piperidine is a common organic compound, it is an immensely important class of compounds medicinally: the piperidine ring is the most common heterocyclic subunit among FDA approved drugs.
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Bridged ring compound refers to any two rings in the compound, which share two non-directly connected carbon atoms, and are classified into bicyclic hydrocarbons, tricyclic hydrocarbons, tetracyclic hydrocarbons, etc. Carbon atoms used in two or more rings are bridgehead carbon atoms, and the bond connecting the bridgehead carbon atoms is called a bridge. Bridged ring compounds are a class of organic compounds that are widely present in nature and usually have important physiological activities, such as the famous anticancer drug paclitaxel and antimalarial drug artemisinin.
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Pyrrolidine, also known as tetrahydropyrrole, is a saturated five-membered heterocyclic ring, which is miscible with water. Pyrrolidine exists in many alkaloids and drug molecules, such as kappa opioids, antagonists of dopamine D4 receptors, and HIV reverse transcriptase inhibitors.
Benzene is an important organic compound with the chemical formula C6H6, and its molecule consists of a ring of 6 carbon atoms, each with 1 hydrogen atom. Benzene is a sweet, flammable, colorless and transparent liquid with carcinogenic toxicity at room temperature, and has a strong aromatic odor. It is insoluble in water, easily soluble in organic solvents, and can also be used as an organic solvent itself. The ring system of benzene is called benzene ring, and the structure after removing one hydrogen atom from the benzene ring is called phenyl. Benzene is one of the most important basic organic chemical raw materials. Many important chemical intermediates can be derived from benzene through substitution reaction, addition reaction and benzene ring cleavage reaction.
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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