A spiro compound is a polycyclic compound in which two monocyclic rings share one carbon atom; the shared carbon atom is called a spiro atom. Spiro compounds have rigid structures, stable structures, and have special properties that general organic compounds do not possess, such as anomeric effect, spiro conjugation and spiro hyperconjugation. Compared with the monocyclic structure or the planar aromatic structure, the spiro structure has a larger three-dimensional structure; the heterocyclic spiro structure is also regarded as the biological isostere of some groups, which can change the drug to a certain extent. The water solubility, lipophilicity, dominant conformation and ADMET properties of the molecule make the optimized lead molecule easier to drug. Therefore, spiro compounds occupy a very important position in drug development.
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Fluorine is the most electronegative element in the periodic table, and the fluorine atom has a small atomic radius, so fluorine-containing organic compounds have many wonderful properties. For example, the introduction of fluorine atoms or fluorine-containing groups into drug molecules can improve the permeability to cell membranes, metabolic stability and bioavailability; in addition, the introduction of fluorine atoms will improve the lipid solubility of the compound and promote its absorption in the body. The speed of delivery changes the physiological effect. In the field of medicinal chemistry, the introduction of fluorine atoms into organic molecules is an important direction for the development of new anticancer drugs, antitumor drugs, antiviral agents, anti-inflammatory drugs, and central nervous system drugs.
Cyclohexane is an organic compound with a chemical formula C6H12. It is a colorless liquid with a pungent odor, insoluble in water, and soluble in most organic solvents such as ethanol, ether, benzene, and acetone. Cyclohexyl fragments are a common structure in both natural and synthetic drugs. It can be used as both core structure and part of achiral side chain.
Tetrahydroisoquinoline is an organic compound with the chemical formula C9H11N. It is classified as a secondary amine, obtained from isoquinoline by hydrogenation. The tetrahydroisoquinoline moiety forms the backbone of several natural, synthetic and semi-synthetic drugs approved for the treatment of cancer, pain, gout and various neurodegenerative diseases.
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