Morpholine contains secondary amine groups and has all the typical reactive characteristics of secondary amine groups. It can react with inorganic acids to form salts, and react with organic acids to form salts or amides, which can be subjected to alkylation reaction, and can also be reacted with ethylene oxide, ketone or Willgerodt reaction. Morpholine is a six-membered ring containing oxygen and nitrogen, and its alkalinity is much lower than that of its parent piperidine. The marketed morpholine drugs are mainly distributed in the fields of tumors, cardiovascular and cerebrovascular diseases, respiratory system diseases, digestive system diseases, infectious diseases and mental disorders.
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Quinolines are an important class of biologically active heterocyclic compounds, and their derivatives usually exhibit a variety of biological activities. They can be used as antimalarial drugs and in the preparation of other antimalarial drugs. Other important activities of quinoline derivatives include inhibitory activity against EGFR-TK and antipsychotic activity. Futhermore, quinoline scaffolds are present in various drug molecules, including the antimalarial drugs aablaquine, chloroquine, mefloquine and primaquine, and the antibacterial agents gatifloxacin, levofloxacin, and moxifloxacin.
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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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